Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR

Anthranilamide-based benzamidine compound 4 and its N-substituted analogs were designed and examined as factor Xa inhibitors using substituted benzamidines as unconventional S4 binding element. A group of N,N-dialkylbenzamidines (11, 17 and 24) have been discovered as potent factor Xa inhibitors with strong anticoagulant activity and promising oral PK profiles.

Graphical abstractAn anthranilamide-based benzamidine and its N-substituted analogs were designed and examined as factor Xa inhibitors, using the N-substituted benzamidines as unconventional S4 binding element. A group of N,N-dialkylbenzamidines have been discovered as potent factor Xa inhibitors with strong anticoagulant activity and promising oral PK profiles.Figure optionsDownload full-size imageDownload as PowerPoint slide