1038548-91-2Relevant academic research and scientific papers
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase
Morwick, Tina,Büttner, Frank H.,Cywin, Charles L.,Dahmann, Georg,Hickey, Eugene,Jakes, Scott,Kaplita, Paul,Kashem, Mohammed A.,Kerr, Steven,Kugler, Stanley,Mao, Wang,Marshall, Daniel,Paw, Zofia,Shih, Cheng-Kon,Wu, Frank,Young, Erick
experimental part, p. 759 - 777 (2010/07/09)
Ahighly selective series of bisbenzamide inhibitors of Rho-associated coiled-coil forming protein kinase (ROCK) and a related ureidobenzamide series, both identified by high throughput screening (HTS), are described. Details of the hit validation and lead generation process, including structure-activity relationship (SAR) studies, a selectivity assessment, target-independent profiling (TIP) results, and an analysis of functional activity using a rat aortic ring assay are discussed. 2009 American Chemical Society.
RHO KINASE INHIBITORS
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Page/Page column 77-78, (2008/12/07)
Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
