Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere

Authors
Fisher, MJ Giese, U Harms, CS Kinnick, MD Lindstrom, TD McCowan, JR Mest, HJ Morin, JM Mullaney, JT Paal, M Rapp, A Ruhter, G Ruterbories, KJ Sall, DJ Scarborough, RM Schotten, T Stenzel, W Towner, RD Um, SL Utterback, BG Wyss, VL Jakubowski, JA
Citation
Mj. Fisher et al., Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere, BIOORG MED, 10(4), 2000, pp. 385-389
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
4
Year of publication
2000
Pages
385 - 389
Database
ISI
SICI code
0960-894X(20000221)10:4<385:FBGBMW>2.0.ZU;2-K
Abstract
6-[4-Amidinobenzoyl]amino]-tetralone acid is a potent antagonist of GPIIb-I IIa. substitution in the meta position of the benzamidine, or replacement w ith a heteroaryl amidine was tolerated in this series. Use of an acyl-linke d 4-alkyl piperidine as an arginine isostere also provided active compounds . Compounds from this series provided substantial systemic exposure in the rat following oral administration. (C) 2000 Elsevier Science Ltd. All right s reserved.