Stereochemistry in drug design discusses the importance of stereochemistry in drug development. It covers different types of stereoisomers like enantiomers and diastereoisomers and geometric isomers. It also discusses the thalidomide disaster and Easson-Stedman hypothesis that differences in biological activity between enantiomers result from selective reactivity of one enantiomer with receptors requiring a three-point fit. Finally, it provides examples of drugs with multiple chiral centers, geometric isomerism, conformational isomers, and acetylcholine.

1. Stereochemistry in drug
design

2. Stereoisomers
• Enantiomers
• Diastereoisomers (includes geometric isomers and ring systems)

4. Thalidomide disaster

5. Stereochemistry and Biologic Activity

6. Easson-Stedman Hypothesis
• In 1933, Easson and Stedman reasoned that differences in biologic
activity between enantiomers resulted from selective reactivity of one
enantiomer with its receptor
• They postulated that such interactions require a minimum of a three-
point fit to the receptor

7. Difference in Vasopressor activity of these molecules

8. Selective phases to which optical isomers can be subjected
before biologic response

9. Drugs with two or more chiral centres

10. Example of Geometric Isomerism

11. Conformational isomers

12. Case of Acetyl Choline