山东大学：《药物化学 Medicinal Chemistry》课程教学资源（PPT课件讲稿）Chapter 01 Introduction（主讲：马淑涛）

Medicinal chemistry Chapter 1 Introduction College of Pharmacy, SDU

Medicinal Chemistry Chapter 1 Introduction College of Pharmacy, SDU

Definition Medicinal chemistry is a chemistry-based discipline, involving aspects of biological, medical and pharmaceutical sciences. It is concerned with the invention, discovery, design, identification and preparation of biologically active compounds, the study of their metabolism, the interpretation of their mode of action at the molecular level and the construction of structure-activity relationships ( sARs)

Definition • Medicinal chemistry is a chemistry-based discipline, involving aspects of biological, medical and pharmaceutical sciences. It is concerned with the invention, discovery, design, identification and preparation of biologically active compounds, the study of their metabolism, the interpretation of their mode of action at the molecular level and the construction of structure-activity relationships (SARs)

In particular, Medicina/ chemistry also involves the discovery of new chemical entities for the treatment of diseases and the systematic study of the structure-activity relationships of the active compounds. Such studies provide the basis for development of better medicinal agents from lead compounds found via random screening, systematic screening and rational design

• In particular, Medicinal chemistry also involves the discovery of new chemical entities for the treatment of diseases and the systematic study of the structure-activity relationships of the active compounds. Such studies provide the basis for development of better medicinal agents from lead compounds found via random screening, systematic screening and rational design

Drug is any substance presented for treating curing or preventing disease in human beings or in animals. It may also be used for making a medical diagnosis or for restoring, correcting or modifying physiological functions

• Drug is any substance presented for treating, curing or preventing disease in human beings or in animals. It may also be used for making a medical diagnosis or for restoring, correcting, or modifying physiological functions

Structure-activity relationship (saR)is the relationship between chemical structure and pharmacological activity for a series of compounds Lead compound is a compound that has a desirable biological activity with therapeutic relevance, but typically has some shortcoming that is likely to be overcome through the development of analogs

• Structure-activity relationship (SAR) is the relationship between chemical structure and pharmacological activity for a series of compounds. • Lead compound is a compound that has a desirable biological activity with therapeutic relevance, but typically has some shortcoming that is likely to be overcome through the development of analogs

Emphasis 1. Chemcially structural feature, physico-chemical property, stability 2. Biological effect adverse effects biotransformation etc 3. Structure-activity relationship, drug targets in living bodies as well as mode of action

Emphasis • 1. Chemcially structural feature, physico-chemical property, stability. • 2.Biological effect, adverse effects, biotransformation etc. • 3. Structure-activity relationship, drug targets in living bodies as well as mode of action

The important role of drugs in human society Drugs have irrevocably changed the fabric of society by improving both the individual quality of life and life expectancy Some examples are shown as follows 9

The important role of drugs in human society • Drugs have irrevocably changed the fabric of society by improving both the individual quality of life and life expectancy. • Some examples are shown as follows:

1. Bacterial and virus infections: polio smallpox, tuberculosis and related diseases have, to a very major extent, become minor public health concerns 2. An increase in life expectancy resulting from drug therapy has also led to a shift in population demographics toward a more healthy, elderly population 3. Drug regimens for birth control have improved individual life choices and the quality of life

• 1. Bacterial and virus infections: polio, smallpox, tuberculosis and related diseases have, to a very major extent, become minor public health concerns. • 2. An increase in life expectancy resulting from drug therapy has also led to a shift in population demographics toward a more healthy, elderly population. • 3. Drug regimens for birth control have improved individual life choices and the quality of life

4. HIv protease and reverse transcriptase inhibitors for the treatment of hiv infections have changed a disease with a fatal prognosis to a potentially chronic one 5. Cancer is also being viewed as a potentially chronic. rather than fatal disease with newer non cytotoxic approaches Notes: H/, Human immunodeficiency virus

• 4. HIV protease and reverse transcriptase inhibitors for the treatment of HIV infections have changed a disease with a fatal prognosis to a potentially chronic one. • 5. Cancer is also being viewed as a potentially chronic, rather than fatal disease with newer, non￾cytotoxic approaches. • Notes: HIV, Human immunodeficiency virus

Section 1 Origins of Medicinal Chemistry 1. Early investigations of natural products 1.1. In the so-called pre-scientific era Natural products having a history as folk remedies were in use. Fore examples, opium belladonna, cinchona bark, etc. Many drugs originally used as folk remedies, nowadays have been abandoned

Section 1 Origins of Medicinal Chemistry 1. Early investigations of natural products • 1.1.In the so-called pre-scientific era • Natural products having a history as folk remedies were in use. Fore examples, opium, belladonna, cinchona bark, etc. Many drugs originally used as folk remedies, nowadays, have been abandoned