Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis

被引：112

作者：

Shanmugavelan, Poovan ^{[1
]}

Nagarajan, Sangaraiah ^{[1
]}

Sathishkumar, Murugan ^{[1
]}

Ponnuswamy, Alagusundaram ^{[1
]}

Yogeeswari, Perumal ^{[2
]}

Sriram, Dharmarajan ^{[2
]}

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 24期

关键词：

1,2,3-Triazoles; 1,3-Dipolar cycloaddition; Antituberculosis; 1,3-DIPOLAR CYCLOADDITIONS; AGENTS; ANALOGS; DERIVATIVES; TRIAZOLES; RESISTANT; TARGETS; ALKYNES; AZIDES; BM212;

D O I：

10.1016/j.bmcl.2011.10.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Efficient and rapid synthesis of 1,2,3-triazole derivatives has been achieved via Huisgen's 1,3-dipolar cycloaddition between alkyl/arylazides and diethyl/dimethyl acetylenedicarboxylate in excellent yields under solvent-free conditions. The environmentally friendly solvent-free protocol overcomes the limitations associated with the prevailing time-consuming solution phase protocols and affords the triazoles just in 1-3 min. In vitro antitubercular activity of these triazoles was screened against Mycobacterium tuberculosis H(37)Rv strain. Four of the compounds showed MIC in the range of 1.56-3.13 mu g/mL proving their potential activity. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7273 / 7276

页数：4

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