Synthesis and biological activity of 4-methyl-3,5-dioxane derivatives as thromboxane A(2) receptor antagonists

Authors
Marusawa, H Setoi, H Kuroda, A Sawada, A Seki, J Motoyama, Y Tanaka, H
Citation
H. Marusawa et al., Synthesis and biological activity of 4-methyl-3,5-dioxane derivatives as thromboxane A(2) receptor antagonists, BIO MED CH, 7(11), 1999, pp. 2635-2645
Citations number
37
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
11
Year of publication
1999
Pages
2635 - 2645
Database
ISI
SICI code
0968-0896(199911)7:11<2635:SABAO4>2.0.ZU;2-E
Abstract
The synthesis and biological activity of novel 4-methyl-3,5-dioxane analogu es are described. All compounds were produced through modification of the s ubstituent formally corresponding to the w-octenol side chain of thromboxan e A(2) (TXA(2)), in reference to the structure of SQ29548. Several compound s were found to be potent TXA(2) receptor antagonists. Compound 8b was the most effective inhibitor of 9,11-epoxymethano PGH(2) (U-46619)-induced huma n platelet aggregation (IC50 = 7.4 nM). (C) 1999 Elsevier Science Ltd. All rights reserved.