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Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold
Ilaš, Janez ; Tomašič, Tihomir ; Kikelj, Danijel
Novel thrombin inhibitors with the central 1,4-benzoxazine-3(4H)-one scaffold,benzamidine P1 arginine side chain mimetic and various P3 moieties are described. ...3-(Benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazi n-7-yl)amino)-3-oxopropanoic acid (7b), the most potent compound in the series, exhibited a Ki of 2.6 nM in vitro for thrombin and high selectivity against trypsin and factor Xa
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