454483-42-2Relevant articles and documents
Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-monocyclic arginine surrogates
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
, p. 1203 - 1208 (2007/10/03)
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-aminopyrazines, and (3) 2-aminopyrimidines and 2-aminotetrahydropyrimidines.
