Chapter 5

Isosteric and Spatial Considerations of Drugs

M. O. Faruk Khan and Timothy J. Hubin

Abstract

This chapter is a brief review of the isosterism and steriochemical principles and their applications in drug action. After study of this chapter, students will be able to: • Define isosterism and bioisosterism of drugs and apply these concepts in drug discovery and drug action • Explain how drugs’ spatial factors control their activity • Define important stereochemical parameters in drugs • Assign drugs stereochemistry and apply those in drug action and receptor binding • Explain the basis of the structure activity relationship and mechanism of drug action

Total Pages: 131-159 (29)

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