Abstract
This chapter is a comprehensive account of the medicinal chemistry of
antihypertensive drugs, Ca2+-channel blockers (CCBs). It provides the mechanism of
drug action and detailed structure-activity relationships (SAR) of the CCBs to give the
knowledge base for pharmacists. After studying this chapter, students will be able to:
• Comprehend the historical background of the CCBs.
• Classify different types of voltage-gated Ca2+ channels (VGCCs) and their clinical
significance.
• Explain CCBs and their clinical significance.
• Describe the mechanisms of action of CCBs at the molecular level including their
binding modes against the VGCCs.
• Describe the SAR of the different classes of CCBs.
• Delineate clinical significance and therapeutic evaluations of these classes of drugs by
solving case studies.
• Articulate the discovery process of a few CCBs.