5651-87-6Relevant articles and documents
Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives
Nagarsenkar, Atulya,Guntuku, Lalita,Guggilapu, Sravanthi Devi,Danthi Bai,Gannoju, Srinivasulu,Naidu,Bathini, Nagendra Babu
, p. 782 - 793 (2016)
In our venture towards the development of effective cytotoxic agents, a panel of triazole linked 3-benzylidene isatin hybrids were synthesized and characterized by IR,1H NMR,13C NMR and Mass spectral analysis. All the newly synthesiz
Synthesis, antimicrobial evaluation and docking studies of oxazolone-1,2,3-triazole-amide hybrids
Kumar, Lokesh,Lal, Kashmiri,Kumar, Aman,Kumar, Ashwani
, p. 5079 - 5097 (2021/09/22)
In an attempt to develop quality antimicrobial agents, a series of oxazolone-1,2,3-triazole-amide hybrids were obtained from oxazolone tethered with a terminal alkyne and in situ generated 2-azido-N-phenylacetamides. All the synthesized compounds were characterized by using various spectroscopic techniques. The developed hybrids were evaluated for their in vitro antimicrobial activity toward three Gram-positive bacteria S. aureus, B. subtilis and S. gorodonii and three Gram-negative bacteria—E. coli, S. enterica and P. aeruginosa—and two fungi, viz. C. albicans and A. niger. Oxazolone-amide-1,2,3-triazoles (8a–e, 9a–e, 10a–e) exhibited almost 15 times better efficacy than alkyne precursors, i.e., oxazolone-linked terminal alkynes (6a–c). Compound 10d exhibited very good antimicrobial activity toward all the tested microorganisms. Docking studies of compounds 10d and 6c were also carried out in the binding site of enzyme sterol-14-α-demethylase of C. albicans, which supported the in vitro experimental results.
Design, synthesis, biological activity, molecular docking and computational studies on novel 1,4-disubstituted-1,2,3-Triazole-Thiosemicarbazone hybrid molecules
Ghule, Vikas D.,Kumar, Ashwani,Kumar, Lokesh,Kumar, Nikhil,Lal, Kashmiri,Naveen,Tittal, Ram Kumar
, (2020/02/29)
A library of some novel 1,4-disubstituted-1,2,3-triazole-thiosemicarbazone hybrid molecules were designed and synthesized from (4-Prop-2-ynyloxy-benzylidene)-thiosemicarbazone and aryl azides under Cu(I)-catalyzed cycloaddition reaction. All newly synthesized [4-(1-Benzyl-1H-[1,2,3]triazol-4-ylmethoxy)-benzylidene] -thiosemicarbazone hybrid molecules were efficiently characterized by IR, 1H NMR, 13C NMR, HRMS and structure of alkynes 3 & 12 were finally supported by X-ray crystallographic data. Compounds 5c, 5d, 9c, 9d 13c and 13d demonstrated excellent potency results for B. Subtilis and P. Aeruginosa bacterial strains with MIC values 0.0141, 0.0152, 0.0562, 0.0608, 0.0141, 0.0608, 0.0141, 0.0304, 0.0281, 0.0304, 0.0281, 0.0304, respectively as compared to reference drug Ciprofloxacin. Antibacterial activity results were supported by molecular docking and DFT studies.
