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- Title
Antiplatelet α-Methylidene-γ-butyrolactones: Synthesis and evaluation of quinoline, flavone, and xanthone derivatives.
- Authors
Wang, Tai-Chi; Chen, Yeh-Long; Tzeng, Cherng-Chyi; Liou, Shorong-Shii; Chang, Ya-Ling; Teng, Che-Ming
- Abstract
As a continuation of our previous studies on the synthesis and antiplatelet activity of coumarin derivatives of α-methylidene-γ-butyrolactones, certain quinoline, flavone, and xanthone derivatives were synthesized and evaluated for antiplatelet activity against thrombin (Thr)-, arachidonic acid (AA)-, collagen (Col)-, and platelet-activating factor (PAF)-induced aggregation in washed rabbit platelets. These compounds were synthesized from quinolin-8-ol, flavon-7-ol, and xanthon-3-ol, respectively, via alkylation and Reformatsky-type condensation ( Schemes 1-3). By the comparison with comparison with coumarin α-methylidene-γ-butyrolactone 3a, flavone and xanthone derivatives, 3b and 3c, respectively, are more selective in which only AA- and collagen-induced aggregation are strongly inhibited. Most of the quinoline derivatives ( 9a-e) exhibited broad-spectrum antiplatelet activities.
- Publication
Helvetica Chimica Acta, 1996, Vol 79, Issue 6, p1620
- ISSN
0018-019X
- Publication type
Article
- DOI
10.1002/hlca.19960790612