- Non-covalent thrombin inhibitors
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The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and which feature a six member heterocyclic ring having two ring nitrogen atoms and the remainder of the ring atoms carbon atoms at P1. These compounds have biologic
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- Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates
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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 ~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.
- 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
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p. 2925 - 2930
(2007/10/03)
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