Synthesis and structure–activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: Application of weakly basic sulfoximine …
A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine
moiety as novel S4 binding element in anthranilamide chemotype has been identified. Lead
optimization at this novel P4 group led to many potent factor Xa inhibitors with excellent
anticoagulant activity in human plasma. Selected compounds were dosed orally in rats and
checked for their ex vivo prothrombin time prolonging activity, which resulted in identification
of compound 5-chloro-N-(5-chloropyridin-2-yl)-2-(4-(N-(2-(diethylamino) acetyl)-S …
moiety as novel S4 binding element in anthranilamide chemotype has been identified. Lead
optimization at this novel P4 group led to many potent factor Xa inhibitors with excellent
anticoagulant activity in human plasma. Selected compounds were dosed orally in rats and
checked for their ex vivo prothrombin time prolonging activity, which resulted in identification
of compound 5-chloro-N-(5-chloropyridin-2-yl)-2-(4-(N-(2-(diethylamino) acetyl)-S …
