1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors

Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability Replacement of the highly basic benzamidine moiety of NAPAP by the moderately...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-03, Vol.9 (5), p.685-690
Hauptverfasser:	Rewinkel, J.B.M., Lucas, H., van Galen, P.J.M., Noach, A.B.J., van Dinther, T.G., Rood, A.M.M., Jenneboer, A.J.S.M., van Boeckel, C.A.A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Anticoagulants - chemical synthesis Anticoagulants - chemistry Anticoagulants - pharmacology Benzamidines - chemistry Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Caco-2 Cells - drug effects Caco-2 Cells - physiology Dipeptides - chemical synthesis Dipeptides - chemistry Dipeptides - pharmacology Drug Design Humans Isoquinolines - chemistry Medical sciences Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Thrombin - antagonists & inhibitors Trypsin Inhibitors - chemical synthesis Trypsin Inhibitors - chemistry Trypsin Inhibitors - pharmacology
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Zusammenfassung:	Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00069-4