Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety

Autor:	Adang, Anton E.P., Lucas, Hans, de Man, Adrianus P.A., Engh, Richard A., Grootenhuis, Peter D.J.
Zdroj:	Bioorganic & Medicinal Chemistry Letters; 1998, Vol. 8 Issue: 24 p3603-3608, 6p
Abstrakt:	Replacement of the noragmatine group in thrombin inhibitors with a ß-alanyl-guanidine group resulted in a nearly equipotent and more selective compound 8 despite the fact that the pKa of this P1 moiety is five orders of magnitude lower. Further modification resulted in a nonpeptide inhibitor with this ß-alanyl-guanidine group, compound 28. This is an active and selective thrombin inhibitor and in view of its nonpeptide/low basicity structure selected for further pharmacological studies.
Databáze:	Supplemental Index
Externí odkaz:	Zobrazit plný text záznamu Full Text from ScienceDirect