Author/Authors :
Ting Su، نويسنده , , Yanhong Wu، نويسنده , , Brandon Doughan، نويسنده , , Kim Kane-Maguire، نويسنده , , Charles K. Marlowe، نويسنده , , James P. Kanter، نويسنده , , John Woolfrey، نويسنده , , Brian Huang، نويسنده , , Paul Wong، نويسنده , , Uma Sinha، نويسنده , , Gary Park، نويسنده , , John Malinowski، نويسنده , , Stan Hollenbach، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
Abstract :
A series of glycolic and mandelic acid derivatives was synthesized and investigated for their factor Xa inhibitory activity. These analogues are highly potent and selective inhibitors against fXa. In a rabbit deep vein thrombosis model, compound 26 showed significant antithrombotic effects (81% inhibition of thrombus formation) at 1.1 μM plasma concentration following intravenous administration.