Non-covalent thrombin inhibitors featuring p 3-heterocycles with P 1-monocyclic arginine surrogates

…, JJ Cui, JZ Ho, KM Reddy, L Mamedova, PH Vu…

Index: Reiner, John E.; Siev, Daniel V.; Araldi, Gian-Luca; Cui, Jingrong Jean; Ho, Jonathan Z.; Reddy, Komandla Malla; Mamedova, Lala; Vu, Phong H.; Lee, Kuen-Shan S.; Minami, Nathaniel K.; Gibson, Tony S.; Anderson, Susanne M.; Bradbury, Annette E.; Nolan, Thomas G.; Semple, J. Edward Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 8 p. 1203 - 1208

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Citation Number: 47

Abstract

Investigations on P2–P3-heterocyclic dipeptide surrogates directed towards identification of an orally bioavailable thrombin inhibitor led us to pursue novel classes of achiral, non- covalent P1-arginine derivatives. The design, synthesis, and biological activity of inhibitors NC1–NC30 that feature three classes of monocyclic P1-arginine surrogates will be disclosed:(1)(hetero) aromatic amidines, amines and hydroxyamidines,(2) 2- ...