Medicinal Chemistry of Drugs Affecting Cardiovascular and Endocrine Systems

Anticoagulants, Antiplatelets and Thrombolytic Agents

Author(s): M. O. Faruk Khan* and A. R. M. Ruhul Amin

Pp: 107-159 (53)

DOI: 10.2174/9789815179729124030007

* (Excluding Mailing and Handling)


This chapter is a comprehensive account of the medicinal chemistry of anticoagulants, antiplatelets and thrombolytic agents and related drugs. It provides the mechanism of drug action and detailed structure-activity relationship (SAR) of the drugs affecting in these clinical areas to give the knowledge base for pharmacists. After studying this chapter, students will be able to:

• Describe the historical background of the anticoagulants, antiplatelets and thrombolytic agents and and related drugs.

• Describe the mechanism of action, pharmacokinetics (PK), and adverse drug reaction (ADR) of the anticoagulants, antiplatelets and thrombolytic agents.

• Explain the physiology and pathophysiology of clotting cascades and identify the components of a blood clot. • Classify major anticoagulant drugs and their structures and binding.

• Discuss in detail the chemistry and SAR of these drugs.

• Distinguish among drugs used as antiplatelets, anticoagulants and fibrinolytic agents.

 • Delineate the clinical significance and therapeutic evaluations of these classes of drugs by solving case studies.

• Explain the discovery process of a few specific drugs in these classes. 

Keywords: Anticoagulant, Antiplatelet, Antithrombin, Direct thrombin inhibitor (DTI), Fibrinolytic, Glycoprotein IIb/IIIa (GPIIb/IIIa) inhibitors, Heparin, Low molecular weight heparin (LMWH), Non-vitamin K antagonist oral anticoagulants (NOACs), P2Y12 receptor antagonists, Pulmonary embolism (PE), Phosphodiesterase (PDE) inhibitors, PAR-1 antagonists, Thrombolytic, Unfractionated heparin (UFH), Venous thromboembolism (VTE), Vitamin K reductase (VKOR), Xa inhibitors.

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