1,2,4-Triazole d-ribose derivatives: Design, synthesis and antitumoral evaluation

A series of novel pyrazolyl‐oxadiazoline derivatives bearing 1,2,4‐triazole moiety 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j, 4k, 4l, 4m, 4n, 4o, 4p were synthesized by schiff bases of 3‐methyl‐1‐phenyl−5‐(1,2,4‐triazole‐1‐yl)‐4‐formylpyrazole 3a, 3b, 3c, 3d and various benzohydroximinoyl chlorides in the presence of Et3N via 1,3‐dipolar cycloaddition reaction. The target products were confirmed by IR, 1H‐NMR, MS, elemental analysis. In addition, the structure of compound 4d was defined by X‐ray crystallography.

Section: Introductionmentioning

confidence: 99%

Synthesis and Characterization of Novel 1,2,4‐oxadiazoline Derivatives Containing Pyrazole Moiety by 1,3‐Dipolar Cycloaddition

Fei

Zhou

Huang

et al. 2016

“…Heterocyclic skeletons serve as ideal scaffolds on which pharmacophores can be appended to yield potent and selective drugs . Among them, triazole and quinoline derivatives play an important role in several biological and pharmacologically active substances such as antimicrobial and anti‐tumor agents . In view of this research and our desire to develop novel sulphonamide structures bearing heterocycle skeleton, we have designed and synthesized a series of new 7‐nitro‐1‐(piperidin‐4‐yl)‐4,5‐dihydro‐[1,2,4]triazolo[4,3‐a]quinoline‐derived sulphonamides and have screened their antimicrobial activity.…”

Section: Introductionmentioning

confidence: 99%

Novel 7‐Nitro‐1‐(Piperidin‐4‐yl)‐4,5‐Dihydro‐[1,2,4] Triazolo[4,3‐a]Quinoline‐Sulphonamide Derivatives as Antimicrobial Agents: Design, Synthesis, and Bio‐Activity

Reddy

et al. 2015

in Wiley Online Library (wileyonlinelibrary.com).In attempt to search for more potent antimicrobial agents, a series of 7-nitro-1-(piperidin-4-yl)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-derived sulphonamides were synthesized. Their structures were established by elemental analyses, IR, and NMR ( 1 H and 13 C) spectral data. The antibacterial activity of the obtained compounds was investigated against different Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacteria and antifungal activity against two fungal strains (Aspergillus niger and Aspergillus clavatus) using disk diffusion method at various concentrations (20, 40, 60, and 80 μg/mL). The study reveals that most of the title compounds showed significant antibacterial and fungal activity when compared with their respective standards streptomycin and griseofulvin.

“…1,2,4‐Triazole is a major five‐membered heterocyclic system, and its derivatives have gained importance as they constitute the structural features of many bioactive compounds . Nowadays, the most frequently used clinical triazoles are fluconazole and itraconazole.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Novel 1,2,4‐oxadiazoline Derivatives Containing Quinoline Moiety by 1,3‐Dipolar Cycloaddition

Huang

Fei

et al. 2014