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(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors

✍ Scribed by Robert A. Galemmo Jr.; John M. Fevig; David J. Carini; Joseph Cacciola; Brian L. Wells; Gregory L. Hillyer; Joseph Buriak Jr.; Karen A. Rossi; Pieter F.W. Stouten; Richard S. Alexander; Richard Hilmer; Lori Bostrom; Matthew M. Abelman; Sheng-Lian Lee; Patricia C. Weber; Charles A. Kettner; Robert M. Knabb; Ruth R. Wexler

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 372 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00525-2

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✦ Synopsis

In this report the structure-activity relationships of a series of novel (N-acyl-N-alkyl)glycyl borolysine thrombin inhibitors are described. This work culminates in the discovery of (N-3phenylpropanoyl-N-phenethyl)glycyl borolysine (12j), a potent, orally active inhibitor with a binding conformation in which the N-phenethyl group occupies the aryl binding pocket of thrombin.

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