Clubbed triazoles: A novel approach to antitubercular drugs

Shiradkar, Mahendra; Kumar, G.V. Suresh; Dasari, Varaprasad; Suresh, T. M.; Akula, Kalyan Chakravarthy; Shah, Rachna

doi:10.1016/j.ejmech.2006.12.001

Cited by 117 publications

(56 citation statements)

References 17 publications

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“…They also investigated them for their antimycobacterial and antimicrobial activities. Many compounds have shown promising activity against tuberculosis [98]. The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development.…”

Section: Antitubercular Activitymentioning

confidence: 99%

Pharmacological significance of triazole scaffold

Kharb

Sharma

Yar

2010

Journal of Enzyme Inhibition and Medicinal Chemistry

469

236

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Section: Antitubercular Activitymentioning

confidence: 99%

Pharmacological significance of triazole scaffold

Kharb

Sharma

Yar

2010

Journal of Enzyme Inhibition and Medicinal Chemistry

469

236

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“…Thiazoles are a familiar group of heterocyclic compounds possessing a wide variety of biological activities, and their usefulness as medicines are well established. Thiazole derivatives are reported to exhibit diverse biological activities as antimicrobial [3][4][5], antioxidant [6], antitubercular [7], and anticonvulsant [8], and anticonvulsant, anticancer [9,10] agents. Moreover, many derivatives of thiazoles are used as selective Cyclooxygenase-2 Inhibitors [11], in addition to their use as 5-HT3 receptor antagonists [12] and as potent and selective acetyl Co-A carboxylase-2 inhibitors [13].…”

Section: Chemistrymentioning

confidence: 99%

Synthesis, Characterization and Molecular Docking of Novel Bioactive Thiazolyl-Thiazole Derivatives as Promising Cytotoxic Antitumor Drug

et al. 2015

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Abstract:Reactions of ethylidenethiocarbohydrazide with hydrazonoyl halides gave 1,3-thiazole or 1,3,4-thiadiazole derivatives according to the type of hydrazonoyl halides. Treatment of ethylidenethiosemicarbazide with hydrazonoyl halides and dimethylacetylene dicarboxylate (DMAD) afforded the corresponding arylazothiazoles and 1,3-thiazolidin-4-one derivatives, respectively. The structures of the synthesized products were confirmed by IR, 1 H-NMR, 13 C-NMR and mass spectral techniques. The cytotoxic activity of the selected products against the Hepatic carcinoma cell line (Hepg-2) was determined by MTT assay indicating a concentration dependent cellular growth inhibitory effect, especially for compounds 14c and 14e. The dose response curves indicated the IC 50 (the concentration of test compounds required to kill 50% of cell population) were 0.54 µM and 0.50 µM, respectively. Confocal laser scanning imaging of the treated cells stained by Rhodamin 123 and Acridine orange dyes confirmed that the selected compounds inhibit the mitochondrial lactate dehydrogenase enzymes. The binding mode of the active compounds was interpreted by a molecular docking study. The obtained results revealed promising cytotoxic activity.

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“…These molecules with a highly electronegative part at the sulfhydryl groups have emerged as new anti-TB compounds. Particularly, Schiff bases derivatives probably due to its ability to increase penetration into the bacterial cell (Shiradkar et al, 2006). Benzimidazole is an important pharmacophore in drug discovery.…”

Section: Azoles Derivativesmentioning

confidence: 99%