Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors was written by Zhang, Han;Liu, Huan;Luo, Xiao;Wang, Yuxi;Liu, Yuan;Jin, Hongwei;Liu, Zhenming;Yang, Wei;Yu, Peilin;Zhang, Liangren;Zhang, Lihe. And the article was included in European Journal of Medicinal Chemistry in 2018.Electric Literature of C7H7ClN2O This article mentions the following:
In this study, a series of novel 2,3-dihydroquinazolin-4(1H)-one derivatives, e.g. I was subsequently synthesized and characterized. Their inhibitory activity against the TRPM2 channel was evaluated by calcium imaging and electrophysiol. approaches. Some of the compounds exhibited significant inhibitory activity, especially 6-bromo-8-methyl-2-[3-(2-naphthyl)-1H-pyrazol-4-yl]-2,3-dihydro-1H-quinazolin-4-one which showed an IC50 of 3.7μM against TRPM2 and did not affect the TRPM8 channel. The summarized structure-activity relationship (SAR) provided valuable insights for further development of specific TRPM2 targeted inhibitors. In the experiment, the researchers used many compounds, for example, 6-Chloro-2-aminobenzamide (cas: 54166-95-9Electric Literature of C7H7ClN2O).
6-Chloro-2-aminobenzamide (cas: 54166-95-9) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Electric Literature of C7H7ClN2O
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics