Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors

A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity of these inhibitors is reported.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (10), p.1069-1072
Hauptverfasser:	Coburn, C A, Rush, D M, Williams, P D, Homnick, C, Lyle, E A, Lewis, S D, Lucas, Jr, B J, Di Muzio-Mower, J M, Juliano, M, Krueger, J A, Vastag, K, Chen, I W, Vacca, J P
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetamides - chemistry Acetamides - pharmacology Aminopyridines - chemistry Aminopyridines - pharmacology Animals Anticoagulants - chemical synthesis Anticoagulants - chemistry Anticoagulants - pharmacology Biological Availability Dipeptides - chemistry Dogs Drug Design Drug Evaluation, Preclinical - methods Humans Molecular Mimicry Pyridones - chemistry Pyridones - pharmacology Rats Structure-Activity Relationship Thrombin - antagonists & inhibitors Thrombosis - drug therapy
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Beschreibung
Zusammenfassung:	A new class of conformationally constrained thrombin inhibitors is described. These compounds contain a unique bicyclic pyridone scaffold which serves as a P3P2 dipeptide surrogate. The synthesis and antithrombotic activity of these inhibitors is reported.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(00)00170-0