Choi-Sledeski, Yong Mi; Kearney, Robert; Poli, Gregory; Pauls, Henry; Gardner, Charles; Gong, Yong; Becker, Michael; Davis, Roderick; Spada, Alfred; Liang, Guyan; Chu, Valeria; Brown, Karen; Collussi, Dennis; Leadley, Robert Jr.; Rebello, Sam; Moxey, Phillip; Morgan, Suzanne; Bentley, Ross; Kasiewski, Charles; Maignan, Sebastien; Guilloteau, Jean-Pierre; Mikol, Vincent published the artcile< Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand>, Category: esters-buliding-blocks, the main research area is ketopiperazino methylazaindole factor Xa inhibitor structure thrombolytic.
The discovery and SAR of ketopiperazino methylazaindole factor Xa inhibitors are described. Structure-activity data suggesting that this class of inhibitors does not bind in the canonical mode were confirmed by an X-ray crystal structure showing the neutral haloarom. bound in the S1 subsite. The most potent azaindole (I, RPR209685) is selective against related serine proteases and attains higher levels of exposure upon oral dosing than comparable benzamidines and benzamidine isosteres. Compound I was efficacious in the canine AV model of thrombosis.
Journal of Medicinal Chemistry published new progress about Crystal structure. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.
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Ester – an overview | ScienceDirect Topics