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

Authors
Rewinkel, JBM Lucas, H van Galen, PJM Noach, ABJ van Dinther, TG Rood, AMM Jenneboer, AJSM van Boeckel, CAA
Citation
Jbm. Rewinkel et al., 1-aminoisoquinollne as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors, BIOORG MED, 9(5), 1999, pp. 685-690
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
685 - 690
Database
ISI
SICI code
0960-894X(19990308)9:5<685:1ABIIT>2.0.ZU;2-0
Abstract
Replacement of the highly basic benzamidine moiety of NAPAP by the moderate ly basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with im proved selectivity towards trypsin and enhanced Caco-2 cell permeability. ( C) 1999 Elsevier Science Ltd. All rights reserved.