606-45-1Relevant articles and documents
Microwave-assisted synthes is of novel chiral receptors derived from deoxycholic acid and their molecular recognition properties
Ye, Ying,Suo, Yourui,Yang, Fang,Han, Lijuan
, p. 1812 - 1814 (2014)
Under microwave irradiation (MWI), novel chiral receptors derived from deoxycholic acid were synthesized by using deoxycholic acid methyl ester as the spacer, and arylhydrazine and amino acids as the arm. Selective recognition properties of these receptors for aromatic amines and D/L-amino acids have been investigated by UV-vis spectral titration and 1H NMR spectral study. The results indicate this type of receptors can form a 1:1 supramolecular complex with an aromatic amine and a 1:2 supramolecular complex with D/L-tryptophan.
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes
Wang, Congcong,Zhang, Yu-Fang,Guo, Shimeng,Zhao, Quan,Zeng, Yanping,Xie, Zhicheng,Xie, Xin,Lu, Boxun,Hu, Youhong
, p. 941 - 957 (2020/11/30)
GPR52 is an orphan G protein-coupled receptor (GPCR) that has been recently implicated as a potential drug target of Huntington's disease (HD), an incurable monogenic neurodegenerative disorder. In this research, we found that striatal knockdown of GPR52 reduces mHTT levels in adult HdhQ140 mice, validating GPR52 as an HD target. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure-activity relationship (SAR) study. Further studies showed that Comp-43 reduces mHTT levels by targeting GPR52 and promotes survival of mouse primary striatal neurons. Moreover, in vivo study showed that Comp-43 not only reduces mHTT levels but also rescues HD-related phenotypes in HdhQ140 mice. Taken together, our study confirms that inhibition of GPR52 is a promising strategy for HD therapy, and the GPR52 antagonist Comp-43 might serve as a lead compound for further investigation.
Br?nsted acid-catalyzed chlorination of aromatic carboxylic acids
Yu, Zhiqun,Yao, Hongmiao,Xu, Qilin,Liu, Jiming,Le, Xingmao,Ren, Minna
supporting information, p. 685 - 689 (2021/04/09)
The chlorination of aromatic carboxylic acids with SOCl2 has been effectively performed by reacting with a Br?nsted acid as the catalyst. Based on this discovery, an efficient catalytic method that is cheaper than traditional catalytic methods was developed. 20 substrates were chlorinated offering excellent yields in a short reaction time. And the SOCl2/Br?nsted acid system has been used in a larger scale preparative reaction. A dual activation mechanism was proposed to prove the irreplaceable system of SOCl2/Br?nsted acid.