Biarylmethoxy isonipecotanilides as potent and selective inhibitors of blood coagulation factor Xa

G Lopopolo, F Fiorella, M de Candia, O Nicolotti…

Index: Lopopolo, Gianfranco; Fiorella, Filomena; De Candia, Modesto; Nicolotti, Orazio; Martel, Sophie; Carrupt, Pierre-Alain; Altomare, Cosimo European Journal of Pharmaceutical Sciences, 2011 , vol. 42, # 3 p. 180 - 191

Full Text: HTML

Citation Number: 16

Abstract

New chloro-substituted biarylmethoxyphenyl piperidine-4-carboxamides were synthesized and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and thrombin. An investigation of effects of the amidine and isopropyl groups attached at the piperidine nitrogen and 5-(halogenoaryl) isoxazol-3-yl groups as biaryl substituents led us to identify new compounds which proved to be selective fXa inhibitors, with inhibition ...