Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors

Add time:08/24/2019    Source:sciencedirect.com

A series of novel, non-basic 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group, was designed and synthesised. Within this series, the N-2-(morpholin-4-yl)-2-oxoethyl derivative 24 was shown to be a potent, selective fXa inhibitor with good anticoagulant activity. Moreover, 24 possessed highly encouraging rat and dog pharmacokinetic profiles with excellent oral bioavailabilities in both species.

We also recommend Trading Suppliers and Manufacturers of (S)-5-(piperidine-1-carbonyl)pyrrolidin-2-one (cas 110958-23-1). Pls Click Website Link as below: cas 110958-23-1 suppliers

Prev:Hydro-de-halogenation and consecutive deprotection of chlorinated N-amido-pyrrolidin-2-ones with Raney-Ni: an effective approach to gabapentin
Next:Oxiranes and Oxirenes: Fused-ring Derivatives☆)