Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2)

…, B Alexander, JY Zhu, WC Guida, E Schönbrunn…

Index: Pireddu, Roberta; Forinash, Kara D.; Sun, Nan N.; Martin, Mathew P.; Sung, Shen-Shu; Alexander, Brian; Zhu, Jin-Yi; Guida, Wayne C.; Schoenbrunn, Ernst; Sebti, Said M.; Lawrence, Nicholas J. MedChemComm, 2012 , vol. 3, # 6 p. 699 - 709

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Citation Number: 21

Abstract

Potent ROCK inhibitors of a new class of 1-benzyl-3-(4-pyridylthiazol-2-yl) ureas have been identified. Remarkable differences in activity were observed for ureas bearing a benzylic stereogenic center. Derivatives with hydroxy, methoxy and amino groups at the meta position of the phenyl ring give rise to the most potent inhibitors (low nM). Substitutions at the para position result in substantial loss of potency. Changes at the benzylic position are ...