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本文报道了14个6-取代苯基-4,5-二氢-3(2H)哒嗪酮和15个6-取代苯基-3(2H)哒嚎酮的合成及其抗电惊活性。其ED50值表明,以2′,4′-二氯苯基-3(2H)哒嗪酮的抗惊作用为最强。构效分析表明,苯环上的取代基对化合物的抗惊活性有明显影响,吸电子取代基和疏水性参数值较大的取代基有利于提高化合物的抗惊活性。
This paper reports the synthesis and anti-shock activity of 14 6-substituted phenyl-4,5-dihydro-3 (2H) pyridazinones and 15 6-substituted phenyl-3 (2H) pyridones. Their ED50 values indicate that the anti-shock effect of 2 ’, 4’-dichlorophenyl-3 (2H) pyridazinone is the strongest. The structure-activity analysis shows that the substituents on the benzene ring have a significant effect on the anti-shock activity of the compounds, and the electron-withdrawing substituents and substituents with larger hydrophobic parameter values are favorable for improving the anti-shock activity of the compounds.