Thrombin plays a wide range of roles in the regulation and maintenance of hemostasis.
Due to its pivotal role in the coagulation cascade, thrombin is an enzyme of significant clinical interest. Inhibition of this multifunctional serine protease has potential implications in the prevention and treatment of thrombotic disorders. Thus, a series of thrombin inhibitors was developed our lab with the intent to maximize potency, selectivity, and oral bioavailability. Non-natural cationic analogues of arginine and lysine serve as the backbone of these novel compounds. The synthesis and analysis of these novel thrombin inhibitors will be discussed.