Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa
A series of thiophene-containing non-amidine factor Xa inhibitors is described. Simple methyl-substituted thiophene analogs were relatively weak inhibitors. However, introduction of hydrophilic substituents at C-4 or C-5 of the thiophene afforded inhibito
Kochanny, Monica J.,Adler, Marc,Ewing, Janice,Griedel, Brian D.,Ho, Elena,Karanjawala, Rushad,Lee, Wheeseong,Lentz, Dao,Liang, Amy M.,Morrissey, Michael M.,Phillips, Gary B.,Post, Joseph,Sacchi, Karna L.,Sakata, Steven T.,Subramanyam, Babu,Vergona, Ron,Walters, Janette,White, Kathy A.,Whitlow, Marc,Ye, Bin,Zhao, Zuchun,Shaw, Kenneth J.
p. 2127 - 2146
(2008/02/01)
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors
Compound 1 was identified by high throughput screening as a novel, potent, non-amidine factor Xa inhibitor with good selectivity against thrombin and trypsin. A series of modifications of the three aromatic groups of 1 was investigated. Substitution of chlorine or bromine for fluorine on the aniline ring led to the discovery of subnanomolar factor Xa inhibitors. Positions on the anthranilic acid ring that can accommodate further substitution were also identified.
Chou, Yuo-Ling,Davey, David D.,Eagen, Keith A.,Griedel, Brian D.,Karanjawala, Rushad,Phillips, Gary B.,Sacchi, Karna L.,Shaw, Kenneth J.,Wu, Shung C.,Lentz, Dao,Liang, Amy M.,Trinh, Lan,Morrissey, Michael M.,Kochanny, Monica J.
p. 507 - 511
(2007/10/03)
Improved Synthesis of Symmetrical and Unsymmetrical 5,11-Methanodibenzodiazocines. Readily Available Nanoscale Structural Units
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Webb, Thomas H.,Wilcox, Craig S.
p. 363 - 365
(2007/10/02)
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