A facile synthesis of carbocycle-fused mono and bis-1,2,3-selenadiazoles and their antimicrobial and antimycobacterial studies

被引：22

作者：

Chitra, Selvam ^{[2
]}

Paul, Nidhin ^{[1
]}

Muthusubramanian, Shanmugam ^{[1
]}

Manisankari, Paramasivam ^{[2
]}

Yogeeswari, Perumal ^{[3
]}

Sriram, Dharmarajan ^{[3
]}

机构：

[1] Madurai Kamaraj Univ, Sch Chem, Dept Organ Chem, Madurai 625021, Tamil Nadu, India

[2] Alagappa Univ, Dept Ind Chem, Karaikkudi 630003, Tamil Nadu, India

[3] Birla Inst Technol & Sci Pilani, Pharm Grp, Med Chem & Antimycobacterial Res Lab, Hyderabad 500078, Andhra Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 11期

关键词：

Oxidative cyclization; 1,2,3-Selenadiazole; Antimicrobial activity; Mycobacterium tuberculosis; MULTIDRUG-RESISTANT TUBERCULOSIS; SELENIUM HETEROCYCLES; BIOLOGICAL-ACTIVITY; ANTIBACTERIAL ACTIVITY; ANTIFUNGAL ACTIVITIES; MDR-TB; DERIVATIVES; AZINES; INFECTIONS; SULFIDES;

D O I：

10.1016/j.ejmech.2011.09.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of mono and bis-1,2,3-selenadiazole derivatives have been synthesized by the oxidative cyclization of mono and bis semicarbazones of 2-(3-oxo-1,3-diarylpropyl)-1-cyclohexanones using selenium(IV) oxide. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against Escherichia coli (ATCC 25922), Staphylococcus aureus (ATCC 11632) and Candida albicans (ATCC 90028) and in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB). Among these compounds, 1,3-di(4-chlorophenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2h) and 3-(4-chlorophenyl)-1-(4-methylphenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2g) were found to be the most active compounds with MIC of 3.3 and 3.5 mu M respectively against MTB. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：5465 / 5472

页数：8

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