Parallel solid-phase synthesis of zatebradine analogues as potential I-f channel blockers

Authors
Bom, A Booth, S Bruin, J Clark, J Miller, S Wathey, B
Citation
A. Bom et al., Parallel solid-phase synthesis of zatebradine analogues as potential I-f channel blockers, BIOORG MED, 11(17), 2001, pp. 2351-2354
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
17
Year of publication
2001
Pages
2351 - 2354
Database
ISI
SICI code
0960-894X(20010903)11:17<2351:PSSOZA>2.0.ZU;2-U
Abstract
The first solid-phase synthesis of zatebradine I and its analogues is repor ted. This has resulted in the preparation of compounds with increased abili ty to reduce the spontaneous beating of isolated guinea-pig atria in a conc entration-dependent manner. One example, 8g, showed a maximum reduction of beating of 80% at 3 muM compared to a reduction of 40% at 3 muM with zatebr adine 1. (C) 2001 Elsevier Science Ltd. All rights reserved.