Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates |
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| Authors: | Cui Jingrong Jean Araldi Gian-Luca Reiner John E Reddy Komandla Malla Kemp Scott J Ho Jonathan Z Siev Daniel V Mamedova Lala Gibson Tony S Gaudette John A Minami Nathaniel K Anderson Susanne M Bradbury Annette E Nolan Thomas G Semple J Edward |
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| Institution: | Department of Medicinal Chemistry, Corvas International, Inc., 3030 Science Park Road, San Diego, CA 92121, USA. |
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| 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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