370864-81-6Relevant articles and documents
Amido-(propyl and allyl)-hydroxybenzamidines: Development of achiral inhibitors of factor Xa
Gong, Yong,Pauls, Henry W.,Spada, Alfred P.,Czekaj, Mark,Liang, Guyan,Chu, Valeria,Colussi, Dennis J.,Brown, Karen D.,Gao, Jingbo
, p. 217 - 221 (2000)
The design, synthesis and SAR of amido-(propyl and allyl)-hydroxybenzamidine coagulation factor Xa inhibitors is described. These achiral inhibitors are selective for fXa vis a vis structurally related serine proteases and are readily prepared in 6-7 linear steps. The most potent member 9j (fXa K(i) = 0.75 nM) is selective (>1000-fold) and an effective anticoagulant in mammalian plasma. (C) 2000 Elsevier Science Ltd. All rights reserved.