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Summary of knowledge points of medicinal chemistry

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Section 1 Introduction

First, the definition and research content of medicinal chemistry

Definition of medicinal chemistry:

Discovering and inventing new drugs;

Synthetic chemical drugs;

Clarify the chemical properties of drugs;

Study the interaction between drug molecules and body cells (biological macromolecules);

Comprehensive discipline, connecting chemistry and life science.

Research contents of medicinal chemistry:

Chemical structure of chemical drugs

physicochemical property

synthetic technique

Structure-activity relationship

In vivo metabolism

Mechanism of action

Ways and methods to find new drugs

Second, the task of medicinal chemistry

1. provides a theoretical basis for the effective use of existing chemical drugs;

Study the relationship between chemical structure and physical and chemical properties

To study the relationship between chemical structure and biological activity

2. To provide advanced and economical methods and processes for the production of chemical drugs;

3. Explore new ways and methods to create new drugs.

Three. Chemical structure and pharmacological activity

A chemical drug is a substance with a certain chemical structure. As long as the chemical structure is determined, its physical and chemical properties are also determined, and it will produce certain biological activities (including toxic and side effects) when it enters the body and interacts with the human body.

Chemical structure →→→→→→→→→ Physical and chemical properties →→→→→ Biological activity/toxic and side effects

Fourth, the name of the drug

Drugs have their own names, including generic names, chemical names and trade names.

1. international generic drug name (INN), also known as generic name.

The name recommended by the World Health Organization (WHO).

New drug developers apply to WHO during the new drug application process.

The generic name of a drug is not protected by patents and administration, but is the name of the active ingredient indicated in all documents, materials, teaching materials and drug instructions.

The name inn has been adopted by all countries in the world.

1. international generic drug name (INN), also known as generic name.

Any manufacturer of this drug can use INN.

It can only be used as the use name of compound ingredients in compound preparations.

The National Pharmacopoeia Committee of China compiled and published the General Names of Drugs in China (CADN), which became the basis for naming drugs in China.

According to the English name, drug properties, chemical structure and pharmacological effects of INN, the Chinese translation of drugs is mainly transliteration, free translation, transliteration or other translation names, which should correspond to English names as much as possible. Long syllables can be shortened, and Chinese names are no more than 5 ~ 6 words, which is easy to pronounce.

2. Chemical name

(1) English chemical name: It is an international common name, and the commonly used naming system is based on the naming system of American Chemical Abstracts (CA) or International Union of Pure and Applied Chemistry (IUPAC).

(R)-2-(N-((2'-( 1H- tetrazole -5- yl)) -[ 1, 1'- biphenyl ]-4- yl) methyl) valeramido) -3- methylbutyric acid.

(2) Chinese chemical names: The Chinese chemical names of drugs recorded in People's Republic of China (PRC) Pharmacopoeia are usually based on the adopted English chemical names. The naming of new compounds can also refer to the naming principles of organic chemistry. The specific naming method is to take the mother name as the main name, then connect the names of substituents or functional groups, and indicate the serial numbers of substituents or functional groups in the specified order. If there are chemicals with stereochemical structure, they should be marked.

(r)-2-[n-[(2'-(5- tetrazolyl) -4- biphenyl] methyl] pentylamino ]-3- methylbutyric acid

Chinese common name: aspirin

English common name: aspirin

Chinese name: 2- (acetoxy) benzoic acid.

3. Trade name

In order to protect their own interests, manufacturers use trade names to protect themselves and strive to improve the reputation of their products when common names cannot be protected. Firms can apply for intellectual property protection.

Diovan

valsartan

(r)-2-[n-[(2'-(5- tetrazolyl) -4- biphenyl] methyl] pentylamino ]-3- methylbutyric acid

Supplementary knowledge points: basic mother nuclear structure, simple and familiar.

Halogen: fluorine, chlorine, bromine, iodine, sodium and potassium.

Primary amine R-NH2, secondary amine R2-NH, tertiary amine R3-N and quaternary ammonium R4-N+.

Tiangan: A 1, B 2, C 3, D 4, E 5, F 6, G 7, Xin 8, N 9, D 10. For simplicity, complex chemical structures usually do not show c and h. But it can also show.

Methyl -CH3, ethyl-CH2 CH3;

N-propyl -CH2CH2CH3, isopropyl (branched) -CH(CH3)2

Benzene (mono-benzene) naphthalene (dinaphthyl) anthracene (trianthrene)

Phenobarbital, phenytoin sodium. Many drug structures contain benzene (supporting skeleton structure). Nabumetone, propranolol.

Furan (oxygen) thiophene (sulfur) pyrrole (nitrogen)

Thiazole imidazole oxazole

Furan (oxygen) thiophene (sulfur) pyrrole (nitrogen)

Thiazole imidazole oxazole

Furan (oxygen) thiophene (sulfur) pyrrole (nitrogen)

Thiazole imidazole oxazole

Furan (oxygen) thiophene (sulfur) pyrrole (nitrogen)

Thiazole imidazole oxazole

Furan (oxygen) thiophene (sulfur) pyrrole (nitrogen)

Thiazole imidazole oxazole

Furan (oxygen) thiophene (sulfur) pyrrole (nitrogen)

Thiazole imidazole oxazole

Azole contains n, sulfur contains s, and evil contains o; Mimi has two.

Quinoline isoquinoline

Benzimidazole benzothiazole