Medicinal Chemistry for Pharmacy Students

Medicinal Chemistry for Pharmacy Students

Volume: 1

Fundamentals of Medicinal Chemistry and Drug Metabolism

The primary objective of this 4-volume book series is to educate PharmD students on the subject of medicinal chemistry. The book set serves as a reference guide to pharmacists on aspects of chemical ...
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Isosteric and Spatial Considerations of Drugs

Pp. 131-159 (29)

M. O. Faruk Khan and Timothy J. Hubin


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


Bioisosterism, Drug receptor interaction, Isoterism, Receptor, Stereochemistry, Structure activity relationships.


Department of Pharmaceutical Sciences and Research, Marshall University School of Pharmacy, Huntington, WV, USA.