1-苯基-3-(2-羟基苯基-5-芳基)-2-吡唑啉的合成与生物活性

Synthesis and Biological Activities of 1-Phenyl-3-(2-hydroxylphenyl)-5-diaryl-2-pyrazoline

研究1-苯基吡唑啉类化合物的合成及其EcMetAP酶活抑制活性。以查尔酮衍生物与苯肼为原料合成啉类化合物。利用IR、1 H NMR和MS对它们进行表征。利用分光光度法测试化合物的EcMetAP酶活性抑制作用,利用生物分子结构分析软件FieldTemplater和FieldAlign计算化合物和已知的EcMetAP酶抑制剂的空间作用力场的相似性。共合成了6个1-苯基-3-(2-羟基苯基-5-芳基)-2-吡唑啉类化合物,但只有化合物5对EcMetAP酶活性有抑制作用,抑制率为31.62%,空间作用力场的相似度为0.615。说明化合物5可作为先导化合物进行结构优化,得到优良的EcMetAP酶抑制活性化合物。

The synthesis and inhibition activities of pyrazoline derivatives were investigated. A pyrazoline derivative was synthesized from a chalcone derivative and phenylhydrazine. The compounds were characterized by IR spectra, MS spectra, and 1H-NMR spectra. Escherichia coli methionine aminopeptidase （EcMetAP） inhibition activities were determined by UV-vis spectroscopy. The similarity of the molecular force field was investigated by FieldTernplater and FieldAlign software. Six 1-phenyl-3-（2-hydroxylphenyl）-5-diaryl-2-pyrazoline derivatives were obtained and characterized. Only compound 5 possessed Ec- MetAP inhibition -activity at a rate of 31.62%. The similarity between the molecular force fields of compound 5 and the EcMetAP inhibitor was 0. 615. Therefore, compound 5 can be used as a lead compound for discovering compounds with good EcMetAP inhibition activities by lead optimization.