88958-20-7Relevant academic research and scientific papers
Primary discovery of 1-aryl-5-substituted-1H-1,2,3-triazole-4-carboxamides as promising antimicrobial agents
Finiuk, Nataliya,Klyuchivska, Olha,Manko, Nazar,Matiychuk, Vasyl,Obushak, Mykola,Pokhodylo, Nazariy,Stoika, Rostyslav
, (2021/08/05)
Three series of novel 1H-1,2,3-triazole-4-carboxamides: 1-aryl-5-alkyl/aryl-1H-1,2,3-triazole-4-carboxamides, 1-aryl-5-amino-1H-1,2,3-triazole-4-carboxamides and 1,2,3-triazolo[1,5-a]quinazoline-3-carboxamides were synthesized via base-mediated click azide reactions. Compounds were evaluated for their antimicrobial activities against primary pathogens: Gram-positive and Gram-negative bacterial strains Escherichia coli, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, as well as fungal strain Cryptococcus neoformans var. grubii and Candida albicans. Compounds exhibiting moderate to good activities were selected for SAR analysis. Several 5-methyl-1H-1,2,3-triazole-4-carboxamides 4d, 4l, 4r, showed potent antibacterial effect against S. aureus. On the contrary, 5-amino-1H-1,2,3-triazole-4-carboxamide 8b and [1,2,3]triazolo[1,5-a]quinazoline-3-carboxamide 9a were active against pathogenic yeast C. albicans. Thus, compound 4l under 1 μM demonstrated 50% growth inhibition against S. aureus. At the same concentration, the compound 9a killed approx. 40% of C. albicans cells. In general, these compounds demonstrated selective action and no significant impact on the viability of human keratinocytes of HaCaT line.
Synthesis of 1H-1,2,3-triazole-4-carbonitriles as building blocks for promising 2-(triazol-4-yl)-thieno[2,3-d]pyrimidine drug candidates
Sekh, Taras V.,Shyyka, Olga Y.,Pokhodylo, Nazariy T.,Obushak, Mykola D.
, p. 3175 - 3186 (2021/08/30)
A new synthetic route leading to functionalized 1H-1,2,3-triazole-4-carbonitriles has been developed. A set of 1-aryl-5-methyl-1H-1,2,3-triazole-4-carbonitriles was obtained in high yields from readily available starting 1H-1,2,3-triazole-4-carboxylic aci
Synthesis of 1-(1-aryl-1H-1,2,3-triazol-4-yl)-β-carboline derivatives
Pohodylo,Matiichuk,Obushak
, p. 275 - 279 (2014/04/17)
Reaction of 5-methyl-1-aryl-1H-1,2,3-triazole-4-carbocylic acid chlorides with tryptamine derivatives afforded substituted 1-aryl-N-[2-(1H-indol-3-yl) ethyl]-5-methyl-1H-1,2,3-triazole-4-carboxamides. At heating these compounds in toluene in the presence of POCl3 and P2O5 Bischler-Napieralski cyclization occurs giving 1-(1-aryl-5-methyl-1H-1,2,3- triazol-4-yl)-4,9-dihydro-3H-β-carbolines that can be transformed into β-carboline and tetrahydro-β-carboline derivatives.
Synthesis and anticancer activity evaluation of new 1,2,3-triazole-4- carboxamide derivatives
Pokhodylo, Nazariy,Shyyka, Olga,Matiychuk, Vasyl
, p. 2426 - 2438 (2014/05/06)
Anticancer screening of several novel 1,2,3-triazoles has been performed. The 1,2,3-triazole derivatives were synthesized from available starting materials according to the convenient synthetic procedures using a multicomponent reaction which gave a wide
The synthesis of some new (S)-1-aryl-N-(1-hydroxy-3-phenylpropan-2-yl)-5- methyl-1H-1,2,3-triazole-4-carboxamide
Shen,Chen,Wu,Dong
, p. 781 - 786 (2013/08/23)
Some new (S)-1-aryl-N-(1-hydroxy-3-phenylpropan-2-yl)-5-methyl-1 H-1,2,3-triazole-4-carboxamides 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j have been synthesized and established by 1H and 13C NMR, IR, MS spectra, CHN analyses, and x-ray
Synthesis of 1,2,4- and 1,3,4-oxadiazoles from 1-aryl-5-methyl-1H-1,2,3- triazole-4-carbonyl chlorides
Obushak,Pokhodylo,Pidlypnyi,Matiichuk
experimental part, p. 1522 - 1527 (2009/06/28)
5-Substituted 2-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazoles were synthesized by reaction of 1-aryl-5-methyl-1H-1,2,3-triazole-4-carbonyl chlorides with the corresponding 5-substituted 1H-tetrazoles. 5-Methyl-1-phenyl-1H-1,2,3-triazole-4-carb
