Medicinal Chemistry

Voltaire (1694-1778) stated, " Therapeutics is the pouring of a drug of which one knows nothing into a patient of whom one knows less."

Medicinal Chemistry is the science that deals with the discovery or design of new therapeutic chemicals and their development into useful medicines.  It may involve synthesis of new compounds, investigations of their relationships between the structure of natural or synthetic compounds and their biological activities, elucidations of their interactions with receptors of various kinds, including enzymes and DNA, the determination of their absorption, transport, and distribution properties, and studies of the metabolic transformations of these chemicals into other chemicals.

Medicinal chemistry, in its crudest sense, has been practiced for several thousand years. Man has searched for cures of illnesses by chewing herbs, berries roots, and barks.  Some of these early clinical trials were quite successful, however, not until the last 100 year has knowledge of the active constituents of these natural sources been known.  The earliest written records of the Chinese, Indian, South American, and Mediterranean cultures described the therapeutic effects of various plant concoctions.

If the approach to drug discovery continued as in ancient times, few diseases would be treatable today.  Natural products make up a small percentage of drugs on the current market.  Typically, when a natural product is found to be active, it is chemically modified in order to improve its properties.  As a result of advances made in synthesis and separation methods and biochemical techniques since the late 1940s, a more rational approach to drug discovery has been possible, namely, one which involves the element of design.

I. II. III. IV. V. VI. VII. VIII. IX. X. XI. XII. XIII. XIV.

Basic Considerations of Drug Activity. Anticancer Drugs. Analgesics and Anti-Inflammatory Agents. Antimicrobial Drugs. Cholinergic Drugs Part 1. Colinergic Drugs Part 2. Adrenergic Drugs. Cardiovascular Drugs. Psychoactive Drugs. Antihistamines and Local Anesthetics. Abused Drugs. Steroids. Natural Drugs. Others.

Drug Development Game  ["Pipeline"] at Searle Healthnet

Tools

- Chimescape Plugin. You must have this to see 3D structures.

- Shockwave plugin.

Special thanks to Shane K. Anderson, who researched the links, designed and produced this medicinal chemistry web.