Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A4 hydrolase aminopeptidase inhibitors was written by Zhang, Fan;Wu, Dang;Wang, Gao-Lei;Hou, Shuang;Ping, Ou-Yang;Huang, Jin;Xu, Xiao-Yong. And the article was included in Chinese Chemical Letters in 2017.Category: amides-buliding-blocks This article mentions the following:
A series of novel 1,2,3-benzotriazin-4-one derivatives I [R = H, 6-O2N, 7-Cl, etc.; X = (CH2)n; n = 0, 1, 2, 3, 4] were designed, synthesized and their inhibitory activities against leukotriene A4 hydrolase aminopeptidase in-vitro were evaluated. Many compounds showed moderate to good activities at the concentration of 10 μmol/L. Among them, compound I [R = 7-Cl; X = (CH2)4 (II)] exhibited the highest inhibitory activity up to 80.6% with an IC50 of 1.30 ± 0.20 μmol/L. The compound II was also tested for the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA4H enzyme by mol. docking was studied. It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study. The relationship between structure and inhibitory activity was also preliminarily discussed. In the experiment, the researchers used many compounds, for example, 2-Amino-4-fluorobenzamide (cas: 119023-25-5Category: amides-buliding-blocks).
2-Amino-4-fluorobenzamide (cas: 119023-25-5) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics