69626-14-8Relevant academic research and scientific papers
Synthesis, molecular docking, and evaluation of antibacterial activity of 1,2,4-triazole-norfloxacin hybrids
Yang, Ping,Luo, Jia-Bao,Wang, Zi-Zhou,Zhang, Li-Lei,Feng, Jin,Xie, Xiao-Bao,Shi, Qing-Shan,Zhang, Xin-Guo
, (2021/09/04)
A series of 1,2,4-triazole-norfloxacin hybrids was designed, synthesized, and evaluated for in vitro antibacterial activity against common pathogens. All the newly synthesized compounds were characterized by Fourier-transform infrared spectrophotometry, p
Molecular docking studies, biological evaluation and synthesis of novel 3-mercapto-1,2,4-triazole derivatives
Ghanaat, Javad,Khalilzadeh, Mohammad A.,Zareyee, Daryoush
, p. 223 - 232 (2020/02/25)
Abstract: Synthesis of bioactive heterocyclic compounds having effective biological activity is an essential research area for wide-ranging applications. In this study, a conventional methodology has been developed for the synthesis of a series of new 3-mercapto-1,2,4-triazole derivatives 4a–f. The purity and structure of the synthesized molecules were confirmed by 1H NMR, 13C NMR and elemental analysis. In addition, the prepared compounds were screened for their anti-proliferative activity against three human cancer cell lines including A549 (lung cancer), MCF7 (breast cancer) and SKOV3 (ovarian cancer) using MTT reduction assay. All the tested compounds demonstrated remarkable cytotoxic activity with IC50 values ranging from 3.02 to 15.37?μM. The heterocyclic compound bearing 3,4,5-trimethoxy moiety was found to be the most effective among the series displaying an IC50 of 3.02?μM specifically against the ovarian carcinoma cancer cell line (SKOV3). Moreover, Annexin V-FITC/propidium iodide staining assay indicated that this compound can induce apoptosis in SKOV3 cells. Furthermore, cell cycle assay showed a significant cell cycle arrest at the G2/M phase in a dose-dependent manner for this compound. The molecular docking results was showed binding modes of potent compound 4d perfectly corroborated the suggestion of binding to the colchicine site. The entire results conclude that 3-mercapto-1,2,4-triazole derivatives can be synthesized by a green method for biological and pharmacological applications. Graphic abstract: New analogs of 3-mercapto-1,2,4-triazole potential derivatives for anti-proliferative activity were synthesized. Cytotoxic activity of all synthesized compounds was evaluated against tree human cancer cell lines: lung (A549), breast (MCF7) and ovarian (SKOV3).[Figure not available: see fulltext.].
Synthesis, Antiproliferative and Antioxidant Activity of 3-Mercapto-1,2,4-Triazole Derivatives as Combretastatin A-4 Analogues
Al-Mansury, Sadiq,Balakit, Asim A.,Alkazazz, Fatin Fadhel,Ghaleb, Rana A.
, p. 556 - 565 (2021/09/28)
Two series of 3-mercapto-1,2,4-triazole derivatives containing alkoxy substituents different in size and position were synthesized and their structures were characterized by FT-IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. The synthesized compounds were assessed for their antiproliferative activity against colon cancer cell line (SW480). The results indicated that the size and position of the alkoxy group significantly influenced the antiproliferative activity. The highest cancer cell growth inhibition values were observed for the compounds containing 3,4,5-trimethoxyphenyl groups in their structures (57.74, 54.14 and 60.70% at 50 μM for compounds 5a, 12b and 14, respectively). The synthesized compounds were also subjected to DPPH protocol for evaluating the antioxidant activity. The results showed that all compounds had moderate to high levels of antioxidant capacity as compared to ascorbic acid as standard, the highest free radical scavenging capacity of 75% was observed for compound 4a at 50 μM.
Solid-phase synthesis of 4,5-disubstituted-1,2,4-triazole-3-thione derivatives based on the resin-bound acylhydrazines
Liu, Zhanxiang,Yi, Yunrui,Zhao, Jinlong,Tang, Mingxue
experimental part, p. 55 - 61 (2011/10/31)
Highly efficient solid-phase synthesis of 4,5-disubstituted-1,2,4-triazole- 3-thiones under mild conditions has been developed. 4,5-Disubstituted-1,2,4- triazole-3-thione derivatives were synthesized from resin-bound acylhydrazines in several steps, provi
