Synthesis of Coumarin Derivatives as Inhibitors of Platelet Aggregation

✍ Scribed by Yeh-Long Chen; Tai-Chi Wang; Kuan-Han Lee; Cherng-Chyi Tzeng; Ya-Ling Chang; Che-Ming Teng

• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: German
• Weight: 510 KB
• Volume: 79
• Category: Article
• ISSN: 0018-019X
• DOI: 10.1002/hlca.19960790308

✦ Synopsis

In a search for the inhibitors of platelet aggregation, certain coumarin derivatives were synthesized and evaluated for antiplatelet activity against thrornbin(Thr)-, arachidonic acid(AA)-, collagen(Co1)-, and platelet-activating-factor(PAF)-induced aggregation in washed rabbit platelets. These compounds were synthesized from 4-hydroxycoumarin (1) or naphthalen-1-01 via alkylation and Refurmatsky-type condensation (Schemes 1-3). Among them, 4-[(2,3,4,5-tetrahydro-4-rnethylidene-5-oxo-2-phenylfuran-2-yl)methoxy]-2~-l-benzopyran-2-one (6b) showed potent antiplatelet effects on AA-and PAF-induced aggregation with Z C , , values of 8.21 and 103.67 UM, respectively (see Tables 1 and2). The antiplatelet potency of 6b against PAF-induced aggregation could be further improved by introducing a proper substituent at the 2-phenyl group of the lactone ring.