STRUCTURE-ACTIVITY-RELATIONSHIPS OF PHOMACTIN DERIVATIVES AS PLATELET-ACTIVATING-FACTOR ANTAGONISTS

Authors
SUGANO M SATO A SAITO K TAKAISHI S MATSUSHITA Y IIJIMA Y
Citation
M. Sugano et al., STRUCTURE-ACTIVITY-RELATIONSHIPS OF PHOMACTIN DERIVATIVES AS PLATELET-ACTIVATING-FACTOR ANTAGONISTS, Journal of medicinal chemistry, 39(26), 1996, pp. 5281-5284
Citations number
13
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
39
Issue
26
Year of publication
1996
Pages
5281 - 5284
Database
ISI
SICI code
0022-2623(1996)39:26<5281:SOPDAP>2.0.ZU;2-K
Abstract
Phomactins, natural products isolated from the culture broth of marine fungus Phoma sp., were found to be active as PAF antagonists. This un ique carbon skeleton led us to investigate the structure-activity rela tionship demonstrating that the lipophilicity at C-(7-8), acetoxy, (me thoxycarbonyl)oxy, and S-isoxazolyloxy substitution at C-20, and 2-bet a-OH configuration at C-2 are all required for the enhancement of inhi bitor activity.