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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, inhibitory activity towards human leukocyte elastase and molecular modelling studies of 1-carbamoyl-4-methyleneaminoxyazetidinones.
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Synthesis, inhibitory activity towards human leukocyte elastase and molecular modelling studies of 1-carbamoyl-4-methyleneaminoxyazetidinones.

机译：合成，对人白细胞弹性蛋白酶的抑制活性和1-氨基甲酰基-4-亚甲基氨基xyazetidinones的分子模型研究。

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摘要

Some monocyclic beta-lactam derivatives of type 3 (MAOAs) in which the leaving group (LG) on the C(4) is a methyleneaminoxy moiety, were synthesised and tested in vitro and in vivo for their inhibitory activity towards human leukocyte elastase (HLE). Some compounds showed an appreciable in vitro inhibitory activity against this enzyme. Effects on the anti-HLE activity due to the nature of the substituents R and R(1) present on their LG were observed and rationalised by means of molecular modelling techniques. The results of in vivo pharmacological tests indicated that MAOAs, while showing an inhibitory activity on the haemorrhage induced by HLE, did not exhibit any effects due to the R and R(1) substituents.
机译：合成了一些3型单环β-内酰胺衍生物，其中C（4）上的离去基团（LG）是亚甲基氨基氧基部分，并在体内和体外测试了它们对人白细胞弹性蛋白酶（HLE）的抑制活性）。一些化合物对这种酶显示出明显的体外抑制活性。通过分子建模技术观察并合理化了由于其LG上存在的取代基R和R（1）的性质对抗HLE活性的影响。体内药理学测试的结果表明，MAOAs虽然对HLE引起的出血具有抑制活性，但由于R和R（1）取代基而没有表现出任何作用。

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