Author/Authors :
Tianbao Lu، نويسنده , , Bruce Tomczuk، نويسنده , , Roger Bone، نويسنده , , Larry Murphy، نويسنده , , F. Raymond Salemme، نويسنده , , Richard M. Soll، نويسنده ,
Abstract :
We expand the structural requirements and structure–activity relationship of a novel class of non-peptidic aryl-based thrombin inhibitors through exploration of the S1 specificity pocket of thrombin using flexible and constrained amidines. The most active compound of this class is 11 with Ki=69 nM, which is ca. 15-fold less potent than constrained guanidine 5.
