| Summary: | 碩士 === 高雄醫學院 === 藥學研究所 === 86 === In a search for inhibitors of platelet aggregation，a
number ofα-met-hylidene-γ-butyrolactone bearing flavones were
synthesized and evaluated for their antiplatelet activity
against thrombin( Thr )-，arachidonic acid( AA )-，collagen( Col
)-，and platelet-activating factor( PAF )-induced aggregation
inwashed rabbit platelets. These compounds were synthesized from
3-hydroxyflavo-ne, 6-hydroxyflavone or 7-hydroxyflavone via O-
alkylation and reformatsky-typecondensation. Most of the
flavone- containing- α-methylidene- γ-butyrolacto-nes showed
potent effects on AA- and Col- induced aggregation . Among them
6-hydroxyflavone derived α- methylidene- γ- butyrolactones
were found to have thirty to one hundred times more potent than
aspirin against AA-induced aggre-gation.
For the vasorelaxingeffects，7-[(2,3,4,5,- Tetrahydro-2-
methyl-4-methylidene-5-oxofuran-2-yl) methoxy]-2-phenyl-4H-1-
benzopyran -4-one was the only compound which exhibited
significant inhibitory activity on the high-K+medium，Ca2+-
induced vasoconstriction and norepinephrine-induced phasic and
tonic constrictions.
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