1737-21-9Relevant articles and documents
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective κ opioid receptor antagonists
He, Guangchao,Peng, Kewen,Song, Qiao,Wang, Junwei,Xu, Anhua,Xu, Yungen,Zhu, Qihua
, (2020/05/19)
Aminobenzyloxyarylamide derivatives 1a-i and 2a-t were designed and synthesized as novel selective κ opioid receptor (KOR) antagonists. The benzoyl amide moiety of LY2456302 was changed into N-hydroxybenzamide and benzisoxazole-3(2H)-one to investigate whether it could increase the binding affinity or selectivity for KOR. All target compounds were evaluated in radioligand binding assays for opioid receptor binding affinity. These efforts led to the identification of compound 1c (κ Ki = 179.9 nM), which exhibited high affinity for KOR. Moreover, the selectivity of KOR over MOR and DOR increased nearly 2-fold and 7-fold, respectively, compared with (±)LY2456302.
Ruthenium(II)-catalyzed synthesis of hydroxylated arenes with ester as an effective directing group
Yang, Yiqing,Lin, Yun,Rao, Yu
supporting information; experimental part, p. 2874 - 2877 (2012/07/28)
An unprecedented Ru(II) catalyzed ortho-hydroxylation has been developed for the facile synthesis of a variety of multifunctionalized arenes from easily accessible ethyl benzoates with ester as an efficient directing group. Both the TFA/TFAA cosolvent system and oxidants serve as the critical success factors in this transformation. The reaction demonstrates excellent reactivity, good functional group tolerance, and high yields.
Compounds containing an amino salicylic acid moiety linked to a sulphapyridine moiety via stable bridge
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, (2008/06/13)
A compound of the formula Het--NR--SO2 --Ph2 --A--Ph1 (COOH)(OH) and tautomeric form, salts, solvates, C1-6 alkyl esters and pharmaceutical compositions of the compound. Ph1 and Ph2 are ben