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. 2002 Oct 21;12(20):2925-30.
doi: 10.1016/s0960-894x(02)00585-1.

Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates

Jingrong Jean Cui  1 , Gian-Luca Araldi, John E Reiner, Komandla Malla Reddy, Scott J Kemp, Jonathan Z Ho, Daniel V Siev, Lala Mamedova, Tony S Gibson, John A Gaudette, Nathaniel K Minami, Susanne M Anderson, Annette E Bradbury, Thomas G Nolan, J Edward Semple
Affiliations

Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates

Jingrong Jean Cui et al. Bioorg Med Chem Lett. .

Abstract

Novel, potent, and highly selective classes of thrombin inhibitors were identified, which resulted from judicious combination of P4-aromatics and P2-P3-heterocyclic dipeptide surrogates with weakly basic (calcd pKa approximately non-basic-8.6) bicyclic P1-arginine mimics. The design, synthesis, and biological activity of achiral, non-covalent, orally bioavailable inhibitors NC1-NC44 featuring P1-indazoles, benzimidazoles, indoles, benzotriazoles, and aminobenzisoxazoles is disclosed.

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