Medicinal Chemistry for Pharmacy Students

Volume: 1

Isosteric and Spatial Considerations of Drugs

Author(s): M. O. Faruk Khan and Timothy J. Hubin

Pp: 131-159 (29)

DOI: 10.2174/9781681086873118010008

* (Excluding Mailing and Handling)


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

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

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