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
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.