83697-74-9Relevant academic research and scientific papers
Synthesis and biological evaluation of 3-amino-1,2,4-triazole derivatives as potential anticancer compounds
Benhida, Rachid,Demange, Luc,Dufies, Maeva,Grytsai, Oleksandr,Hagege, Anais,Martial, Sonia,Pagès, Gilles,Penco-Campillo, Manon,Ronco, Cyril,Valiashko, Oksana
, (2020/10/02)
Two series of compounds carrying 3-amino-1,2,4-triazole scaffold were synthesized and evaluated for their anticancer activity against a panel of cancer cell lines using XTT assay. The 1,2,4-triazole synthesis was revisited for the first series of pyridyl derivatives. The biological results revealed the efficiency of the 3-amino-1,2,4-triazole core that could not be replaced and a clear beneficial effect of a 3-bromophenylamino moiety in position 3 of the triazole for both series (compounds 2.6 and 4.6) on several cell lines tested. Moreover, our results point out an antiangiogenic activity of these compounds. Overall, the 5-aryl-3-phenylamino-1,2,4-triazole structure has promising dual anticancer activity.
Antitubercular activities of the novel synthesized 1,2,4-triazole derivatives
Oh, Taegwon,Hayat, Aisal,Yoo, Euna,Cho, Sang-Nae,Sheen, Yhun Yhung,Kim, Dae-Kee,Choo, Hea-Young Park
, p. 43 - 51 (2015/03/04)
1,2,4-Triazoles exert antimycobacterial activity by inhibiting the cell wall biosynthesis. In an attempt to developing lead compounds exhibiting antitubercular activities, a series of 1,2,4-triazole derivatives were synthesized by introducing various substitutes into a scaffold and the antitubercular activity was evaluated. The most potent compounds 3e and 8d showed their minimum inhibitory concentrations against Mycobacterium tuberculosis as 12.5 ??M. The results indicate that those compounds can be considered as leads for further development of new 1,2,4-triazole type candidates with high antitubercular activities.
Design and synthesis of N-Aryl isothioureas as a novel class of gastric H+/K+-ATPase inhibitors
Ma, Chao,Wu, Anhui,Wu, Yongqi,Ren, Xuhong,Cheng, Maosheng
, p. 891 - 900 (2014/01/06)
To find new H+/K+-ATPase inhibitors for the treatment of peptic ulcer disease, a series of novel N-aryl isothiourea derivatives were synthesized and their structures were identified by 1H NMR and GC-MS. The effects of these compounds on inhibiting gastric acid secretion were evaluated by the guinea pig stomach mucous membrane study with pantoprazole magnesium as a positive control. The results showed that, of the 37 N-aryl isothiourea compounds synthesized, 20 compounds have comparable or stronger gastric acid inhibitory activities than that of pantoprazole magnesium. The quantitative structure-activity relationships (QSARs) of the N-aryl isothiourea compounds were also studied by comparative molecular field analysis (CoMFA) computation, and the model structure that was supposed to give more powerful bioactivities was finally predicted. A series of novel N-aryl isothiourea derivatives were synthesized and evaluated for their effects of inhibiting gastric acid secretion using the guinea pig stomach mucous membrane study with pantoprazole magnesium as a positive control. Compounds 2c, 2e, and 2k have higher bioactivity. The quantitative structure-activity relationships also defined these structural requirements.
