Synthesis and SAR of pyridazinone-substituted phenylalanine amide α4 integrin antagonists
Structural modification and cellular adhesion inhibition activities of pyridazinone-substituted phenylalanine amide α4 integrin antagonists are described. Functionality requirements for the arylamide moiety and the carboxylic acid group were de
The compounds of the present invention are novel bicyclic triazole amino acid-derivatives useful as a4 integrin receptor antagonists. The invention is further directed to methods for treating integrin mediated disorders including, but not limited to, infl
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Page/Page column 46
(2008/06/13)
Synthesis and biological evaluation of novel pyridazinone-based α4 integrin receptor antagonists
A novel series of pyridazinone-functionalized phenylalanine analogues was prepared and evaluated for inhibition of cellular adhesion mediated by α4β1/VCAM-1 and α4β 7MAdCAM-1 interactions. Concise syntheses were
Gong, Yong,Barbay, J. Kent,Dyatkin, Alexey B.,Miskowski, Tamara A.,Kimball, Edward S.,Prouty, Stephen M.,Fisher, M. Carolyn,Santulli, Rosemary J.,Schneider, Craig R.,Wallace, Nathaniel H.,Ballentine, Scott A.,Hageman, William E.,Masucci, John A.,Maryanoff, Bruce E.,Damiano, Bruce P.,Andrade-Gordon, Patricia,Hlasta, Dennis J.,Hornby, Pamela J.,He, Wei
p. 3402 - 3411
(2007/10/03)
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