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《ACTA PHARMACEUTICA SINICA》 1999-01
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SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6 (4′ SUBSTITUTED ACYLAMINOPHENYL) 4,5 DIHYDRO 3 (2H) PYRIDAZINONES

Liu Chaomei(Liu CM), Xue Kechang(Xue KC), Yao Jiayong(Yao JY), Jiang Yuanying(Jiang YY), Lu Bo(Lu B) and Wu Yijie(Wu YJ) (Division of Organic Chemistry, Faculty of Pharmacy, Second Military Medical University, Shanghai 200433)  
AIM: To study the synthesis and antiplatelet aggregation activity of 6 (4′ substituted acyl aminophenyl) 4,5 dihydro 3(2H) pyridazinones. METHODS: The title compounds were synthesized by acylation of twelve acyl chlorides and two intermediates prepared by Friedel Crafts reaction, lengthening of carbon chain, hydrolysis and cyclization; the antiplatelet aggregation activity of the title compounds was measured by Born′s method. RESULTS: Twenty four 6 (4′ substituted acyl aminophenyl) 4,5 dihydro 3(2H) pyridazinones were designed and synthesized. Of them, 22 were first reported. The chemical structures of all the compounds were determined by IR, 1HNMR and elementary analysis. The intermediate, 6 (4′ aminophenyl) 4,5 dihydro 3(2H) pyridazinones, was synthesized by two methods. Preliminary pharmacological tests showed that all of the title compounds inhibited ADP induced platelet aggregation to a certain extent. Compounds II showed more potent inhibition than did compounds I. The inhibitory activities of I 1, I 3, II 1, II 3, II 4, II 6 and II 9, were more potent than that of the control compound CI 930. The inhibitory effect of II 1 and II 3 against platelet aggregation were about ten times of that of CI 930. CONCLUSION: Some of the title compounds showed potent activity of antiplatelet aggregation and should be studied further.
【CateGory Index】: R914.5
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