Non-covalent thrombin inhibitors featuring P 3-Heterocycles with P 1-Bicyclic arginine surrogates

…, DV Siev, L Mamedova, TS Gibson, JA Gaudette…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 20 p. 2925 - 2930

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被引用次数: 23

摘要

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, ...