This chapter presents a comprehensive account of the medicinal chemistry
of drugs affecting the renin-angiotensin system (RAS). It provides the mechanism of
drug action and details structure-activity relationships (SAR) of the drugs affecting
RAS to give the knowledge base for pharmacists. After studying this chapter, students
will be able to:
• Describe the historical background the RAS and drugs acting on this system.
• Explain RAS enzymes and hormones and their roles in blood pressure.
• Classify drugs acting on the RAS and their structures and binding.
• Discuss in detail the chemistry and SAR of the antagonists involved in RAS including
angiotensin-converting enzyme inhibitors (ACEIs), angiotensin receptor blockers
(ARBs) and renin inhibitors.
• Delineate the clinical significance and therapeutic evaluations of these classes of
drugs by solving case studies.
• Explain the discovery process of ACEIs and ARBs.
Keywords: ACE, ACEIs, ARBs, Drug receptor interaction, Renin inhibitor, RAS, Structure-activity relationship.
