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一些新型4-(4'-取代苯基)-6-(4''-羟基苯基)-2-(取代亚氨基)嘧啶的合成、抗病毒、抗结核和抗菌活性

Synthesis, antiviral, antituberculostic and antibacterial activities of some novel, 4-(4'-substituted phenyl)-6-(4"-hydroxyphenyl)-2-(substituted imino) pyrimidines.

作者信息

Siddiqui Anees A, Rajesh Ramadoss, Alagarsamy Veerachamy, Meyyanathan Subramania N, Kumar Bommenahalli P, Suresh Bhojraj

机构信息

Department of Pharmaceutical Chemistry, Jamia Hamadard, Hamdard University, New Delhi-110 62, India.

出版信息

Acta Pol Pharm. 2007 Jan-Feb;64(1):17-26.

Abstract

A variety of novel 4-[(4'-substituted phenyl)-6-(4"-hydroxyphenyl)-2-substituted imino] pyrimidines were synthesized by reacting 4-(4'-substituted phenyl)-6-(4"-hydroxyphenyl)-2-aminopyrimidines with different substituted aromatic aldehydes, with coumarin and with chloroisatin. The 4-(4'-chlorophenyl)-6-(4"-hydroxyphenyl)-2-aminopyrimidines were synthesized by reacting 3-(4'-substituted phenyl)-1-(4"-hydroxyphenyl)-2-propen-1-ones with guanine hydrochloride. The 3-(4'-substituted phenyl)-1-(4"-hydroxyphenyl)-2-propen-1-ones were synthesized by reacting 4-hydroxyacetophenone with different para substituted aromatic aldehydes. Spectral data (IR, NMR, and mass spectra) confirmed the structures of the synthesized compounds. The synthesized compounds were investigated for their antiviral, antituberculostic and antibacterial activities. The results indicated that the synthesized compounds have mild to potent activities with reference to their appropriate reference standards. However, mechanism related studies could be carried out to predict the structure activity relationship for all the compounds.

摘要

通过使4-(4'-取代苯基)-6-(4''-羟基苯基)-2-氨基嘧啶与不同的取代芳醛、香豆素和氯异靛红反应,合成了多种新型的4-[(4'-取代苯基)-6-(4''-羟基苯基)-2-取代亚氨基]嘧啶。通过使3-(4'-取代苯基)-1-(4''-羟基苯基)-2-丙烯-1-酮与盐酸鸟嘌呤反应,合成了4-(4'-氯苯基)-6-(4''-羟基苯基)-2-氨基嘧啶。通过使4-羟基苯乙酮与不同的对取代芳醛反应,合成了3-(4'-取代苯基)-1-(4''-羟基苯基)-2-丙烯-1-酮。光谱数据(红外光谱、核磁共振光谱和质谱)证实了合成化合物的结构。对合成的化合物进行了抗病毒、抗结核和抗菌活性研究。结果表明,相对于适当的参考标准,合成的化合物具有轻度至强效的活性。然而,可以进行与作用机制相关的研究,以预测所有化合物的构效关系。

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