要芬梅, 孙常晟. 6-取代二氢哒嗪酮类化合物的合成及血小板聚集抑制作用J. 药学学报, 1993, 28(7): 548-552.
引用本文: 要芬梅, 孙常晟. 6-取代二氢哒嗪酮类化合物的合成及血小板聚集抑制作用J. 药学学报, 1993, 28(7): 548-552.
FM Yao, CS Sun. SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6-SUBSTITUTED DIHYDROPYRIDAZINONESJ. Acta Pharmaceutica Sinica, 1993, 28(7): 548-552.
Citation: FM Yao, CS Sun. SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6-SUBSTITUTED DIHYDROPYRIDAZINONESJ. Acta Pharmaceutica Sinica, 1993, 28(7): 548-552.

6-取代二氢哒嗪酮类化合物的合成及血小板聚集抑制作用

SYNTHESIS AND PLATELET AGGREGATION INHIBITORY ACTIVITY OF 6-SUBSTITUTED DIHYDROPYRIDAZINONES

  • Abstract: In order to develop more potent and less toxic, antithrombotic agents, ten 6-(4-substituted piperazinyl acetyl aminophenyi)-4, 5-dihydro-3(2H)-pyridazinones were synthesized. The title compounds were tested in vitro for platelet aggregation inhibitory activity with ADP-induced rat platelets and PAF-induced rabbit platelets. Preliminary tests showed that all of the pyridazinones could inhibit ADP-induced rat platelet aggregation. Ⅰ7, Ⅰ8, Ⅰ9 were more potent than the control compound CI 930. Ⅰ9 was the most potent compound with IC50 of 0.99 μmol/L. Pertaining to PAF-induced rabbit platelet aggregation. Ⅰ9 was the most potent inhibitor with IC50 of 3.7 μmol/L.

     

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