3296-02-4Relevant articles and documents
Mechanisms involved in the antinociceptive and anti-inflammatory effects of a new triazole derivative: 5-[1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole (LQFM-096)
Cardoso, Carina S.,Silva, Daiany P. B.,Silva, Dayane M.,Florentino, Iziara F.,Fajemiroye, James O.,Moreira, Lorrane K. S.,Vasconcelos, José P.,Sanz, Germán,Vaz, Boniek G.,Li?o, Luciano M.,Lima, Danilo da S.,dos Santos, Fernanda Cristina A.,Menegatti, Ricardo,Costa, Elson A.
, p. 877 - 892 (2020)
The aim of this study was to design, synthesize and evaluate the potential analgesic and anti-inflammatory effects of 5-[1-(4-fluorphenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole—(LQFM-096: a new triazole compound) as well as to elucidate its possible mechani
Synthesis and rational design of new appended 1,2,3-triazole-uracil ensembles as promising anti-tumor agents via in silico vegfr-2 transferase inhibition
Bhaskar, Kuthati,Hu, Anren,Hung, Sung-Jen,Raju, Atcha Krishnam,Rao, Vankadari Srinivasa,Reddy, Nadipolla Naresh,Reddy, Puchakayala Muralidhar,Rohini, Rondla,Sanjeev, Ananthula,Swamy, Merugu Kumara
, (2021/05/29)
Angiogenesis inhibition is a key step towards the designing of new chemotherapeutic agents. In a view to preparing new molecular entities for cancer treatment, eighteen 1,2,3-triazole-uracil ensembles 5a–r were designed and synthesized via the click reaction. The ligands were well characterized using1 H-,13 C-NMR, elemental analysis and ESI-mass spectrometry. The in silico binding propinquities of the ligands were studied sequentially in the active region of VEGFR-2 using the Molegro virtual docker. All the compounds produced remarkable interactions and potentially inhibitory ligands against VEGFR-2 were obtained with high negative binding energies. Drug-likeness was assessed from the ADME properties. Cytotoxicity of the test compounds was measured against HeLa and HUH-7 tumor cells and NIH/3T3 normal cells by MTT assay. Compound 5h showed higher growth inhibition activity than the positive control, 5-fluorouracil (5-FU), against both HeLa and HUH-7 cells with IC50 values of 4.5 and 7.7 μM respectively. Interestingly, the compounds 5a–r did not show any cytotoxicity towards the normal cell lines. The results advance the position of substituted triazoles in the area of drug design with no ambiguity.
Triazole [5, 4-d] pyrimidone tricyclic compounds as well as preparation method and application thereof
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Paragraph 0064; 0067-0070; 0073, (2021/07/09)
The invention relates to triazole [5, 4-d] pyrimidone tricyclic compounds as well as a preparation method and application thereof.The triazole [5, 4-d] pyrimidone tricyclic compounds are prepared by following steps: taking different substituted anilines a