What is Medicinal Chemistry?

Medical chemistry (Medicinal chemistry) refers to a discipline that uses chemical concepts and methods to discover, confirm and develop drugs, and studies how drugs work in the body at the molecular level.

Medicinal Chemistry is a discipline based on chemistry and biology that studies the structure and activity of drugs. The research involves discovering, modifying and optimizing lead compounds, revealing the mechanism of action of drugs and physiologically active substances at the molecular level, and studying the metabolic processes of drugs and physiologically active substances in the body.

Chinese name: Medicinal chemistry
Foreign name: Medicinal chemistry
Foundation: Chemistry and biology

Research object: For drug structure and activity
Content: Discover, modify and optimize lead compounds
Task: Obtain new chemical entities to create new drugs

Basic introduction to medicinal chemistry

Medicinal chemistry task

Investigate the relationship between the chemical structure and activity of drugs (structure-activity relationship); the relationship between the chemical structure of drugs and physicochemical properties; elucidate the interaction between drugs and receptors; identify the absorption, transport, distribution and metabolites of drugs in vivo New chemical entities are created through drug molecule design or chemical modification of lead compounds.

Object of medicinal chemistry research

Including drugs (drugs) and related substances and general physiologically active substances, the main research object is drugs.

Medicinal Chemistry is a comprehensive discipline that discovers and invents new drugs, synthesizes chemical drugs, clarifies the chemical properties of drugs, and studies the interaction laws between drug molecules and body cells (biomacromolecules). Leading discipline. Medicinal chemistry is a classic science with a long history. It has a solid foundation for development, has accumulated a wealth of content, and has made important contributions to human health.

Medicinal chemistry

Research content of medicinal chemistry

It mainly includes two points: 1. Drugs with known pharmacological effects and clinical application, including their preparation methods. Analyze and confirm quality control, structural transformation, and the relationship between chemical structure and pharmacological activity. 2. Design and innovate drugs from the perspective of biology and chemistry, mainly study the physical and chemical process of drug-organism interaction, and reveal the mechanism and mode of action of drugs from the molecular level.

In short, the main task of medicinal chemistry is to explore and research and discover new high-efficiency, low-toxicity and health-friendly drugs, which is also the driving force for the development of medicinal chemistry.

Development of medicinal chemistry

The development of medicinal chemistry in this century can be summarized into several stages. At the end of the 19th century, the rise of the chemical industry and the establishment of the Ehrlich concept of chemotherapeutics laid the foundation for the synthesis and progress of chemical drugs at the beginning of the century. For example, early organic drugs containing antimony and arsenic were used to treat trypanosomiasis, amoebiasis, and syphilis. On this basis, the development of chemical drugs for the treatment of malaria and parasitic diseases.

After the discovery of Bailangduoxi and sulfa in the mid-1930s, a series of sulfa drugs were synthesized. In 1940, the efficacy of penicillin was affirmed, and -lactam antibiotics developed rapidly. The scope of chemotherapy is expanding, and it is no longer limited to bacterial infections. With the establishment of the woods and FildeS antimetabolism theory in 1940, it not only clarified the mechanism of action of antibacterial drugs, but also opened up new ways for finding new drugs. For example, antitumor drugs, diuretics, and antimalarials have been discovered based on antimetabolism. Research on the relationship between drug structure and biological activity has also been carried out, providing an important basis for the creation of new drugs and leaders. The largest number of chemical drugs were discovered in the 1930s and 1940s. This period was a bumper era in the history of medicinal chemistry development.

After entering the 1950s, the number of new drugs was not as good as the initial stage. The mechanism of action and metabolic changes of the drug in the body were gradually clarified, leading to the connection of physiology, biochemical effects and the search for new drugs for the cause. Improved the pharmacophore or basic structure of the drug Ways to find new medicine. For example, the concept of latentiation and prodrug is used to design new compounds that can reduce toxic and side effects and increase selectivity. After the discovery of chlorpromazine for schizophrenia in 1952, the treatment of mental and neurological diseases achieved breakthrough progress. Non-steroidal anti-inflammatory drugs have been an active area of research since the mid-1960s, and a series of new anti-inflammatory drugs have been marketed.

Medicinal chemistry Structure-effect relationship research has developed rapidly since the 1960s, and has changed from qualitative to quantitative. Quantitative structure-activity relationship (QSAR) is to analyze and calculate the structural information, physical and chemical parameters and biological activity of compounds, establish a reasonable mathematical model, study the quantitative change law between structure and effect, and provide a theory for drug design and guide the structural transformation of lead compounds in accordance with. Common methods for QSAR include Hansch linear multiple regression model, Free-WilSon addition model, and Kier molecular connectivity. Most of the parameters used are measured by the two-dimensional structure of the compound, which is called two-dimensional quantitative structure-activity relationship (2D-QSAR). The 1950s to 1960s were an important period for the development of medicinal chemistry. From the 1970s to the present, in-depth research has been conducted on potential targets of drugs, and their structure and function have been gradually understood. In addition, the penetration of molecular mechanics and quantum chemistry and pharmaceutical sciences, the application of X-ray diffraction, biological nuclear magnetic resonance, databases, and molecular graphics, in order to study the three-dimensional structure of drugs and biological macromolecules, the conformation of pharmacodynamics, and the mode of action of the two, explore the structure-effect The relationship provides theoretical basis and advanced means. The combination of SD-QSAR and structure-based design methods will make drug design more rational.

After the use of norfloxacin in the clinic in the early 1980s, it quickly set off a wave of research on quinolone antibacterials. A series of antibacterials have been synthesized successively. The advent of such antibacterials and some new antibiotics is considered to be important in the development history of synthetic antibacterials milestone.

Among the new drugs marketed since the early 1990s, biotechnology products account for a large proportion and have a rapid upward trend. Through the transformation of biotechnology, the traditional pharmaceutical industry can increase economic benefits, and the development and production of medicines using transgenic animal-mammary gland bioreactors will be one of the hotspots in the field of biotechnology in the 21st century. The combination chemistry technology developed today can synthesize a large number of structurally related compounds, establish an orderly diversity of molecular libraries, and perform intensive and rapid screening. Such large-scale synthesis and high-throughput screening are undoubtedly useful for discovering lead compounds and improving new drugs. The research level is of great significance.

In the 1970s and 1990s, new disciplines formed by new theories, new technologies, and interdisciplinary cross-disciplinaries all promoted the development of medicinal chemistry. It is considered to be a key era in which medicinal chemistry is inherited from the past.

Development status of medicinal chemistry

The progress of medicinal chemistry in the mid and late 20th century and the large number of new drugs coming to market are summarized into three main reasons: (l) the advances in life sciences, such as structural biology, molecular biology, molecular genetics, genetics, and biotechnology. New medicines provide theoretical basis and technical support. (2) The rapid advancement of information science, such as the establishment of bioinformatics, the development of biochips, the application of various information databases and information technology, can easily retrieve and search the required documents. The data, research level and efficiency have been greatly improved; (3) In order to win the international market, pharmaceutical companies have invested heavily in research and development of new drugs (R% 26amp; D), and the number of new drug products has continued to increase, which has promoted the rapid development of the pharmaceutical industry.

Soon we will usher in a new century of knowledge economy. Knowledge innovation, technological innovation, promoting scientific and technological progress and economic development will be the main tasks facing. Life science and information science will be increasingly developed. It will become an active field in the next century, which will provide an important basis for disease prevention and treatment and new drug research. The close integration of medicinal chemistry with biology and biotechnology and mutual promotion will still be the general trend of development in the future.

Pharmaceutical chemical structural transformation

Medicinal chemistry purpose

1. Improve the selectivity of the drug to the target site: the antitumor drug phosphoestrol-diethylstilbestrol SMZ--N-acyl-glutamyl derivative.

3 Prolong the action time of the drug: Prodrug fluphenazine is made with testosterone in oil.

4 Improve drug absorption: increase bioavailability and increase fat solubility.

5. Improve the solubility of the drug: Acyclovir is made into a prodrug, phenytoin, into an ester.

6. Reduce drug side effects: increase selectivity, extend half-life, and improve bioavailability.

7. Play a drug compatibility role.

Medicinal chemistry

Chemical methods are often used for structural modification: semi-synthetic methods are simple and easy, but the structural amplitude is limited; total synthetic methods have a longer route, but can greatly change the structure, and combined chemical methods are convenient for high-throughput screening. Structural modification also uses methods such as biosynthesis and biotransformation of precursors, as well as biological methods such as genetic engineering, cell engineering, and combined biosynthesis. According to needs and possibilities, a variety of structural modifications are made to different antibiotics to expand the antibacterial spectrum, enhance antibacterial activity, overcome resistance, and improve pharmacokinetic properties (such as enhancing stability, increasing blood concentration, and extending elimination half-life ), Reducing toxic and side effects, and adapting to the needs of preparations have achieved great results.

Salt-forming modification: suitable for drugs with acidic and basic groups

1. Salt-forming modification of acidic drugs.

2. Salt-forming modification of basic drugs: Fatty amino groups are strongly alkaline to form inorganic acid salts, and aromatic amino groups are weakly used as organic acid salts to reduce toxicity.

Ester and amide formation

1. Esters with carboxyl group: ibuprofen naproxen.

2. Esters with hydroxyl group: can extend the half-life of the drug metronidazole erythromycin.

3 Amino-forming amides: increase the tissue-selective lysostatin carbamoylation of the drug to azamethine puromycin mitomycin.

Carbonyl drugs, ring-opening, ring-forming modification

1. Screening of lead compounds from natural resources: 3. Lead compounds found in active metabolites: Diazepam Butepine. 2. Combinatorial chemistry 4. Lead compounds were discovered during the research of life-based processes.

Research directions in medicinal chemistry

1. Structure identification and structure-activity relationship study of active ingredients of natural medicine: Study on extraction, isolation, structure identification and activity of active ingredients in plants produced in Northeast China. Studies on the synthesis and structure-activity relationship of natural medicines. Research on anticancer, antiviral, antihyperlipidemic, cardiovascular and cerebrovascular diseases drugs.

2. Study on chemical composition of natural medicine and its biological activity: The main objective is to study natural medicinal chemistry, and the monomer compound component is obtained through extraction, separation, and purification, and the structure is identified by spectroscopy and chemical means; lead compounds with biological activity and Effective parts; research and development of innovative drugs.

3 Research on the chemical composition and biological activity of traditional Chinese medicine: The research content includes extraction, separation, and structural identification of active ingredients in traditional Chinese medicine. The focus is on the chemical composition of new medicinal parts and effective parts of Changbai Mountain Road medicinal materials. Biological activity research is mainly in

Medicinal chemistry Research on the prevention and treatment of anti-cancer, bacteriostasis, treatment of diabetes, hyperlipidemia, cardiovascular diseases, etc.

4 Targeted drug system research: In order to enable drugs to be better absorbed, improve drug bioavailability, and achieve optimal therapeutic effects, design and research targeted drug systems, so that drugs can be combined with or embedded in carriers to form Mobility in the body is a drug delivery system that targets the target tissue to release the drug, that is, the use of a carrier drug release system to change the kinetic process of the drug, that is, to mainly change the distribution of the drug in the body, so that the drug acts only on the target cells of the diseased site, and is avoided Effect on normal cells. The drug is allowed to release one or more drugs in a specific part of the body at a predetermined rate within a specific time, and the metabolic rate of the drug can be controlled.

5. Structure identification and structure-activity relationship study of natural medicines: Taking Chinese unique Chinese herbal medicine and natural products as the main research objects, comprehensive application of the latest theoretical and experimental techniques of chemistry (mainly spectroscopy technology) and biology, and research findings It is possible to develop lead compounds for new drugs and carry out related basic theoretical research.

Major discoveries in medicinal chemistry

In the late 19th century, there was a rush to find chemicals with medicinal value. Paul Ehrlich (1854-1915) was one of the most passionate explorers of chemotherapy. Although his research work dates back to the 1870s, his main contributions did not apply until the 20th century. When Erich was a student in Breslau and Leipzig, he became very interested in dyes and their effect on living tissues. His cousin Carl Weigert (1845-1905) taught him the technique of staining bacteria. Wiggert was not the first to use a colored compound as a biological colorant; chromic acid, magenta, and hematoxylin were used for the same in 1875 before Wiggert stained with methyl violet to show bacteria in animal tissues. The purpose of the method has been more than 10 years. Various staining methods developed rapidly among bacteriologists and histologists. Robert Koch (1843--1910) used the bacterial response to dyes as a tool to identify different bacteria. H.C.J. Gram introduced the identification technology he used in 1884, and many other scientists made Made further contributions.

Based on the selectivity of specific dyes for certain bacteria or tissues, Ehrlich came up with the insight that using the right dyes to treat diseases should be possible. He demonstrated in 1887 that methylene blue can stain living nerve cells without affecting adjacent tissues. Similarly, it can stain certain bacteria without affecting other bacteria. Is it possible to find certain dyes that can attach to a particular organism, thereby killing the organism without damaging the host organism's cells?

In 1889 Elich became a member of the Koch Institute for Infectious Diseases in Berlin. When Emil von Behring (1854-1917) discovered the anti-toxin for diphtheria in 1892, he had established a close relationship with E. von Behring. Elich has a lot to do with the development of serum. He later became director of the National Serum Institute in Frankfurt am Main. Although he has been busy with serum production and experiments all day, he continues his efforts to find a dye that is both highly specific to pathogens and relatively non-toxic to higher animals. He got the cooperation from the Casile Chemical Plant to provide him with samples of new compounds produced in their laboratory. In addition, since the establishment of the Georg Speyer-Haus company in 1906, he was able to place himself among a group of assistants, chemists and bacteriologists, to perform compound synthesis and modification work, and to study Effects and effects of these compounds on pathogens and animals.

Medicinal chemistry At the early stage, Erich proposed his theory of bactericidal side chains. According to this theory, it should be possible to design a molecule with a side chain and have a complementary effect on a certain parasite. This molecule is attached to the microorganism by a side chain method. May hinder the activity of microorganisms or may kill microorganisms. Since these side chains will only act on pathogenic objects without harming host cells, it will be feasible to design these effective magic bullets. His ideas were partly influenced by the success of serum therapies. Here the pathogen itself stimulates the formation of particularly active substances that kill the pathogen without harming most host cells. Because it is impossible to create many effective sera to treat many diseases, it is necessary to develop chemotherapy to produce compounds with specific effects that can kill parasitic bacteria.

Because a chemical that is toxic to an organism will almost certainly show toxicity to other cells, Erich has proposed therapeutic index as a safety standard to ensure the use of chemicals. The index is essentially The ratio of the highest dose that the host animal can tolerate to the effective therapeutic dose.

New discoveries in medicinal chemistry

As early as the early 20th century, Erich and Shiga (Qing). (Jie) discovered that trypanosomal red has special effects on the treatment of diseases caused by trypanosomes. F.E.P. Mesnil and Maurice Nicolle proved that trypan blue is more effective. These drugs have had some success in treating tropical diseases such as sleeping sickness and equine trypanosomiasis. In 1906, Koch used p-aminophenylhydrazone to treat human diseases caused by trypanosomes. The compound was successfully prepared by Bechamp in 1863 and is believed to be acylanilide of arsenic acid. In 1905, Liverpool doctors H.W.Thomas and A.Breinl announced in their report that the compound had a toxic effect against trypanosomes; therefore, p-aminophenylhydrazone (non-toxic to Atoxyl) was used. A name because it is not toxic to the host. Erich knew that arsenic and nitrogen belonged to the same group of elements in the periodic table, so he was very interested in arsenic compounds; he confirmed that the compound had an effect on trypanosomes, but found that it could not be used because it was too toxic to damage Optic nerve. He expressed doubts about the chemical structure of p-aminophenylhydrazone prepared by Bechamp, and proposed the correct structure of the compound. Because he has extensive practical experience with dyes, he also proposed that a free amino group would appear in the structure.

Around this time, Treponema pal-lidum, the organism that caused syphilis, was discovered by Hoffmann and Fritz Schaudinn. Schottin points out that the organism (a spirochaete) is more protozoan-like than bacterial. Elich designed some new arsenic compounds that could be tested in rabbits and mice with these diseases. Starting from the point that the azo group is a curative unit in dyes such as cone red, he used inference to assume that trivalent arsenic may be more effective than pentavalent arsenic, as found in p-aminophenylhydrazone. . His chemist, Alfred Bertheim, prepared these compounds; he found that alastin (paracetamol) was a particularly effective substance in experiments for trypanosomiasis. Compound No. 418, phenylglycine, proved to be more effective. More compounds were synthesized in the laboratory and tested under the guidance of his Japanese assistant, Sahachiro Hata. In 1909, the treatment of syphilis with compound 606 was successful. The drug was later sold on the market under the name Salfossan or Vanamin. Later in 1912, a more convenient compound, 914, was developed. Therapies using these arsenic preparations were quickly introduced. Although Xinsaerfosan is not without its shortcomings, before the 1940s, during the period when effective antibiotics were not used to treat syphilis, it has been the standard medicine for treating this disease. The success of arsenic-containing preparations as a potent drug has brought people a very optimistic mood. It is believed that the chemical industry can make similar various chemotherapeutics. But all enthusiasm turned into disappointment. Because the results of research on those compounds that have curative effects do not make people know how to synthesize various molecules, so that it has specific effects on some diseases without harming the host. With the exception of Bayer 205 and several other compounds, there was little real success in developing chemotherapeutics between 1910 and 1930.

Bayer 205, Germanic Manning, was adopted in 1920 as a specific medicine for African sleeping sickness. Germanic Bayer (the company s U.S. branch was seized and forced to change to an independent company during World War I) obtained these drugs under severe restrictions and was charged as Medicine has been used as a political weapon to help Germany regain lost colonies. Ernest Fourneau (1872-1949) at the Pasteur Insti-tute, despite the lack of patent rights and Bayer's refusal to provide medicine for his research Several compounds have been identified. A group of scientists, together with the British Dye Company, also played an active role in solving the above-mentioned difficult problems. By consulting pre-war German patent literature, Forno learned that they had done a lot of research on complex urea derivatives. There is further evidence in these published patent documents that there is now a great interest in bonding aminobenzoyl and naphthylamine benzenesulfonic acid end groups by some amides, just as there is interest in trypanosomal dyes. After excluding a few hundred possible compounds through one test analysis, the scope was narrowed down to 25, and each compound was tested synthetically and biologically and chemically. One of them, Forno 309, has been proven to have the trypanicidal ability of Bayer 205, non-toxic and chemically stable. Compared with the 56mg German product managed by the Pasteur Institute, the results show that the two compounds are exactly the same, and the Germans refuse to admit that the two compounds are the same; Forno 309 receives patent rights in the UK and the US The compound has a significant effect on early sleeping sickness, but it is powerless against late sleeping sickness. In 1919, Walter Abraham Jacobs and Michael Heidelberger of the Rockefeller Institute of Medicine demonstrated that trypanosomal arsenide is effective in the treatment of advanced sleepiness affecting the central nervous system.

Development Trend of Medicinal Chemistry

The formation and development of any discipline are inseparable from the scientific and technological level and economic construction requirements of the time and the promotion of related disciplines. Early medicinal chemistry was dominated by chemistry, including the nature, preparation methods, and quality testing of natural and synthetic drugs. With the development of science and technology, disciplines such as natural medicinal chemistry, synthetic medicinal chemistry, and medicinal analysis have been established. Modern medicinal chemistry is a comprehensive discipline that interpenetrates chemistry and biology. The main task is to create new drugs and discover leaders with further research and development prospects.

The main research contents are: based on the drug action targets (receptors, enzymes, ion channels, nucleic acids, etc.) revealed by life science research, referring to the structural characteristics of natural ligands or substrates, and designing new drug molecules in order to find selective effects New drugs for raking; finding leaders through various approaches and technologies, such as the discovery of endogenous active substances, the structural modification and optimization of natural active ingredients or existing drugs, the discovery of active metabolites, etc., followed by computers in drug research The applications in the field are becoming more and more extensive, and computer-aided drug design (CADD) and structure-activity relationship are also the research contents of medicinal chemistry. With the rapid development of information science, the use of various databases and information technologies, such as Reaxys, can extensively collect literature on medicinal chemistry, which is conducive to expanding ideas, expanding horizons, and enriching the content of medicinal chemistry.

In order to complete its task, medicinal chemistry needs to study the structure, properties, and changes of chemical drugs, as well as understand the physiological and biochemical effects and toxic and side effects of drugs used in the human body, as well as the structure-activity relationship. Someone likened that if modern medicinal chemistry is a tripod, then the tripod is supported by chemistry, biology and computer technology. The creation of new drugs is an exploratory system engineering involving multiple disciplines and multiple links. It is the result of collective research. Based on medicinal chemistry, we must first find the precursors and provide a material basis for subsequent discipline research. Therefore, it plays a very important role in the research process. Medicinal chemistry is a leader in the field of pharmaceutical science. Burger's famous book "Medicinal Chemistry" has now been changed to (Medicinal Chemistry and Drug Discovery) to highlight the task of medicinal chemistry is to create new drugs and discover leaders, so as to promote the development of the pharmaceutical industry and protect human health the goal of.

In addition, the penetration of molecular mechanics and quantum chemistry and pharmaceutical sciences, the application of X-ray diffraction, biological nuclear magnetic resonance, databases, and molecular graphics, in order to study the three-dimensional structure of drugs and biological macromolecules, the conformation of pharmacodynamics, and the mode of action of the two, and explore the structure The relationship provides theoretical basis and advanced means. It is now believed that the combination of SD-QSAR and structure-based design methods will make drug design more rational. In-depth research on receptors, especially the discovery of many receptor subtypes, has promoted the development of receptor agonists and straw resists, and looking for drugs that specifically act only on a certain receptor subtype can improve its selectivity. For example, and adrenergic receptors and their subtype blockers are commonly used drugs for the treatment of cardiovascular diseases; histamine H2 receptor blockers can treat gastric and duodenal ulcers. Endogenous enkephalins have agonistic effects on opioid receptors, and thus exhibit analgesic activity. Today, there are multiple subtypes of opioid receptors (such as , etc.) which open up the way to design specific analgesics.

With the in-depth study of the three-dimensional structure and active site of enzymes, great progress has been made in the study of enzyme inhibitors based on enzymes. For example, angiotensin mercury-converting enzyme (ACE) inhibitors that achieve hypotensive effects by interfering with the regulation of the Renin-Angiotensin-Aldosterone system are antihypertensive drugs developed in the mid-1970s. medicine. A series of ACE inhibitors such as captopril and enalapril lisinopril are already important drugs for the treatment of hypertension and heart failure. 3Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor has a good curative effect on the prevention and treatment of atherosclerosis and blood lipids. Ticlopidine inhibits thromboxane synthase · Used to prevent and treat thrombosis. Ion channels are similar to activated enzymes that exist in various tissues of the body and are involved in regulating a variety of physiological functions. A series of calcium antagonists (Calcium Antagonists) discovered at the end of the 1970s are important cardio-cerebral vascular medicines. Among them, dihydropyridine is more deeply studied and there are more varieties, each with pharmacological characteristics. The discovered KT regulators have opened a new way to find antihypertensive, antiatrial and class I antiarrhythmic drugs. Cell canceration is thought to be caused by gene mutations that lead to dysregulated gene expression and infinite cell proliferation. Therefore, oncogenes can be used as a point of reference, and antisense technology can be used to inhibit cell proliferation. New anticancer drugs can be designed.

Many active peptides and cytokines such as atrial natriuretic peptide (ANF) were isolated from rat myocardial homogenate in the early 1980s. They have strong diuretic, antihypertensive and rhythm-regulating effects. Endothelial relaxing factor (EDRF) NO is a substance that has been shown to have vasodilating action secreted by endothelial cells at the same time, and its chemical nature has been confirmed to be nitric oxide (Ho). It is a cell messenger molecule that regulates the functions of the cardiovascular system, nervous system and immune system, and participates in various physiological functions of the body. After the 1990s, research on NO has become an international hot spot. The research on NO donors and NO synthase inhibitors is in the ascendant. It will open up new fields for cardiovascular anti-inflammatory drugs.

Biotech products account for a large proportion of new drugs that have been on the market since the early 1990s, and have a rapid upward trend. The transformation of traditional pharmaceutical industry through biotechnology can improve economic benefits. The use of genetically modified animals, the development and production of mammary gland bioreactors will be one of the hot topics in the field of biotechnology in the 21st century.

The developed combinatorial chemistry technology can synthesize a large number of knot-related compounds, establish an orderly changing diversity of molecular libraries, and perform intensive fast structure-speed screening. Such large-scale synthesis and high-throughput screening will undoubtedly lead to the discovery and improvement of lead compounds. The research level of new drugs is of great significance. From the 1970s to the 1990s, new theories, new technologies, and interdisciplinary interdisciplinary emerging disciplines all promoted the development of medicinal chemistry. It is considered to be a key era in which medicinal chemistry is inherited from the past.

The progress of medicinal chemistry and the large number of new drugs on the market in the middle and later stages of this century can be summarized into three main reasons: (l) the progress of life sciences, such as structural biology, molecular biology, molecular genetics, genetics, and biotechnology. New drugs provide theoretical basis and technical support. (2) The rapid advancement of information science, such as the establishment of bioinformatics, the development of biochips, the application of various information databases and information technology, can easily retrieve and search the required security documents. The data, research level and efficiency have been greatly improved. In order to win the international market, pharmaceutical companies have invested a lot and invested funds in new drug research and development (R & D). The number of new drug products has continued to increase, which has promoted the rapid development of the pharmaceutical industry.

Introduction to textbooks of medicinal chemistry

I. Introduction to the discipline of medicinal chemistry

Medical Chemistry (Medicinal Chemistry) is a discipline designed, synthesized, and studied for the prevention, diagnosis, and treatment of drugs based on a variety of chemistry and biology disciplines. Research involves the discovery, development, and identification of new drugs, as well as explaining the mechanism of action of drugs and biologically active compounds at the molecular level. In addition, medicinal chemistry also involves the research, identification, and synthesis of metabolites of drugs and their related compounds.

Medicinal chemistry The medicinal chemistry part mainly includes the drug name, chemical structure, physical and chemical properties, and structure-activity relationship, etc. It is an important part of the necessary pharmaceutical professional knowledge for practicing pharmacists.

Medicinal chemistry basic requirements

1. Grasp the names, chemical names, chemical structures, physical and chemical properties, uses, and structure-activity relationships of important drugs.

2. Grasp the chemical changes that may occur during storage and the relationship between their chemical structure and stability; to ensure that the medication is safe and effective.

3. Grasp the metabolism-related chemical changes and biological activity of some important drugs in the body.

4. Familiar with the stereochemical structure, biological activity characteristics and nomenclature of drugs that are supplied with optically active substances.

5. Familiar with the name, chemical name, chemical structure and use of new drugs on the market.

6. Understand the development history and latest progress of various drugs.

7. Understand some structural factors that affect drug efficacy, the purpose and method of chemical modification of drugs, and the methods and methods of new drug development.

Introduction to textbooks of medicinal chemistry

There are two types of textbooks or reference books for "medical chemistry" in circulation on the market: one is the introduction of tampering with new drug research and development as the main content; Biology and pharmacology knowledge, they emphasize that the subject of medicinal chemistry is a textbook for the development of new drugs; the latter is to introduce the chemical nature of drugs, chemical characteristics, chemical changes in vivo and in vitro, drug molecules and collective mechanisms Textbooks of the nature of chemistry. The former is mainly used to train researchers, so it is more suitable as a teaching book for graduate students, while the latter is mainly suitable for undergraduates majoring in pharmacy, and also provides basic medicinal chemistry knowledge for related majors.

The above classification of auxiliary materials for medicinal chemistry is in the same vein as many other disciplines, and is a process that follows objective laws. Standing on the shoulders of giants, even greater achievements. Knowing "why is this" and "how to do it" has a natural feel.