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按类型衍化出的先导物结构,经逐步调整苯环上取代基的电性和疏水性,合成了45个呋喃、吡咯和N-甲基吡咯-α-甲醛缩N~4-3-,或4-取代的苯基氨脲和氨硫脲。对抗溃疡作用和毒性作用的定量评价及构效分析表明,活性与疏水性呈抛物线关系;引入推电子基团,有利于抗溃疡活性。化合物17和30的活性与毒性的分离较大,其药理作用在深入研究中。
45 kinds of furan, pyrrole and N-methylpyrrole-α-carbaldehyde condensation N ~ 4-3- were synthesized by gradually adjusting the electric and hydrophobic properties of the substituents on the benzene ring according to the structure of the lead derivative. 4-substituted phenylurea and thiourea. Quantitative evaluation and structure-activity analysis of the anti-ulcer effect and toxicity showed that there was a parabolic relationship between activity and hydrophobicity. The introduction of an electron-donating group was beneficial to anti-ulcer activity. Compound 17 and 30 activity and toxicity of the larger separation, its pharmacological effects in-depth study.