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.
