193096-41-2Relevant academic research and scientific papers
Amidino protease inhibitors
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, (2008/06/13)
Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
Non-peptidic phenyl-based thrombin inhibitors: Exploring structural requirements of the S1 specificity pocket with amidines
Lu, Tianbao,Tomczuk, Bruce,Bone, Roger,Murphy, Larry,Salemme, F. Raymond,Soll, Richard M.
, p. 83 - 85 (2007/10/03)
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 K(i) = 69 nM, which is ca. 15-fold less potent than constrained guanidine 5.
