Highly active and selective anticoagulants: D-Phe-Pro-Arg-H, a free tripeptide aldehyde prone to spontaneous inactivation, and its stable N-methyl derivative, D- …

…, E Szell, D Bagdy, E Barabas, G Horvath…

文献索引：Bajusz; Szell; Bagdy; Barabas; Horvath; Dioszegi; Fittler; Szabo; Juhasz; Tomori; Szilagyi Journal of Medicinal Chemistry, 1990 , vol. 33, # 6 p. 1729 - 1735

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被引用次数: 201

摘要

D-Phe-Pro-Arg-H sulfate (GYKI-14166) is a highly active and selective inhibitor of thrombin both in vitro and in vivo. Recent studies on the stability of D-Phe-Pro-Arg-H in neutral aqueous solution at higher temperature have revealed that it is transformed into inactive 5, 6, 8, 9, 10, 10a-hexahydro-2-(3'-guanidinopropy1)-5-benzy1-6-oxo-imidazo [1, 2-a] pyrrolo [2, 1-c] pyrazine. No such inactivation could be observed with Boc-DPhehArg-H (GYKI-lMl) ...