2011
DOI: 10.1016/j.bmcl.2011.10.048
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Efficient synthesis and in vitro antitubercular activity of 1,2,3-triazoles as inhibitors of Mycobacterium tuberculosis

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Cited by 95 publications
(34 citation statements)
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“…In this regard, and in continuation of our recent reports on the solvent-free synthesis of amides [1920], thioamides [21], cyclic imides [22], thiazolidin-4-ones [23], spirothiazolidin-4-ones [24], 1,2,3-triazoles [25], 1,2,3-triazolylchalcones [26], and 1,2,3-triazolyldihydropyrimidine-2-thiones [27], we herein present a one-pot solvent/scavenger-free synthetic protocol for 2-iminothiazolidin-4-ones. This environmentally benign method avoids toxic organic solvents and acid scavengers, the details of which are presented below.…”
Section: Introductionmentioning
confidence: 75%
“…In this regard, and in continuation of our recent reports on the solvent-free synthesis of amides [1920], thioamides [21], cyclic imides [22], thiazolidin-4-ones [23], spirothiazolidin-4-ones [24], 1,2,3-triazoles [25], 1,2,3-triazolylchalcones [26], and 1,2,3-triazolyldihydropyrimidine-2-thiones [27], we herein present a one-pot solvent/scavenger-free synthetic protocol for 2-iminothiazolidin-4-ones. This environmentally benign method avoids toxic organic solvents and acid scavengers, the details of which are presented below.…”
Section: Introductionmentioning
confidence: 75%
“…Preparation of 1,2,3-triazoles by copper-catalysed alkyne-azide cycloaddition (CuAAC) has emerged as a prominent "Click" chemistry [9][10][11]. 1,2,3-Triazoles have received considerable attention in synthetic organic chemistry due to their numerous biological and pharmaceutical activities such as anti-HIV [12][13][14], antibacterial [15][16][17], and antiallergic [18] properties.…”
Section: Introductionmentioning
confidence: 99%
“…AcOH at ambient temperature) allowed for the desired trisubstituted triazoles. For example, triazole 19, which is itself a potent antitubercular agent, 29 could be obtained from diethyl acetylenedicarboxylate and benzyl azide in quant. conversion and with a yield of 90% (entry 19).…”
Section: Resultsmentioning
confidence: 99%