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
The Design of Potent, Selective and Drug-Like RGD αvβ1 Small-Molecule Inhibitors Derived from non-RGD α4β1 Antagonists
Up to 45 % of deaths in developed nations can be attributed to chronic fibroproliferative diseases, highlighting the need for effective therapies. The RGD (Arg-Gly-Asp) integrin αvβ1 was recently investigated for its role in fibrotic disease, and thus war
Hatley, Richard J. D.,Barrett, Tim N.,Slack, Robert J.,Watson, Morag E.,Baillache, Daniel J.,Gruszka, Anna,Washio, Yoshiaki,Rowedder, James E.,Pogány, Peter,Pal, Sandeep,Macdonald, Simon J. F.
supporting information
p. 1315 - 1320
(2019/07/09)
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 present invention relates to certain novel compounds of Formula (I): methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of integrin mediated disorders.
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Page/Page column 38-39
(2010/02/13)
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