BMY-44621

The synthesis and biol. activity of a new series of dipeptide arginine aldehydes with non-amino acid P3 residues are reported.These compounds were designed as thrombin inhibitors to address the role of the P3 amino group in D-Phe-Pro-Arg-H series.Preliminary structure activity relationships are also discussed.The lead candidate in this series is the reversible inhibitor BMY 44621 (I), which is stable in aqueous medium and also exhibits in vitro and ex vivo anticoagulant and in vivo antithrombotic activities.