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

…, PJM Van Galen, ABJ Noach, TG Van Dinther…

Index: Rewinkel; Lucas; Van Galen; Noach; Van Dinther; Rood; Jenneboer; Van Boeckel Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 5 p. 685 - 690

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Citation Number: 45

Abstract

Download full text in PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... 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. ... Stüber, W.; Dickneite, G.; Koschinski, R. DE 4115468, 1992.