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

J.B.M. Rewinkel, H. Lucas, P.J.M. Galen, van, A.B.J. Noach, T.G. Dinther, van, A.M.M. Rood, A.J.S.M. Jenneboer, C.A.A. Boeckel, van

Research output: Contribution to journalArticleAcademicpeer-review

62 Citations (Scopus)

Abstract

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.
Original languageEnglish
Pages (from-to)685-690
JournalBioorganic and Medicinal Chemistry Letters
Volume9
Issue number5
DOIs
Publication statusPublished - 1999

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