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
• 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.