Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa |
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| Authors: | Gong Y Pauls H W Spada A P Czekaj M Liang G Chu V Colussi D J Brown K D Gao J |
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| Institution: | Department of Medicinal Chemistry, Rhone-Poulenc Rorer, Collegeville, PA 19426-0107, USA. |
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| Abstract: | 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 Ki = 0.75 nM) is selective (>1000-fold) and an effective anticoagulant in mammalian plasma. |
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