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从单环β-内酰胺不同类型结构探讨所设想的β-内酰胺酶抑制剂的作用模式.先合成2个系列36个新的单环β-内酰胺化合物,经元素分析、IR、PMR及MS证实.用化学法测试其抑酶活性.鼻子化学CNDO/2法进行分子静电势计算.所得分子静电势图与青霉烷砜酸所得相比较,阐明作用模式设想有合理性.继又合成21个新化合物,也经元素分析、IR、PMR及MS证实.经酶法测试活性,支持了所提出的受体作用模式.
From the different types of monocyclic β-lactams, we explored the mode of action of the envisaged β-lactamase inhibitors.A series of 36 new monocyclic β-lactam compounds were synthesized and analyzed by elemental analysis, IR, PMR and MS confirmed by the chemical method to test its inhibition of enzyme activity CNDO / 2 nasal chemical molecular electrostatic potential calculation of the resulting molecular electrostatic potential obtained penicillin alkanesulfonic acid compared to clarify the mode of action is reasonable to assume. Twenty-one new compounds, also confirmed by elemental analysis, IR, PMR and MS, were tested for enzymatic activity to support the suggested mode of action of the receptor.