50551-58-1Relevant articles and documents
Polysubstituted Pyrimidines as mPGES-1 Inhibitors: Discovery of Potent Inhibitors of PGE2 Production with Strong Anti-inflammatory Effects in Carrageenan-Induced Rat Paw Edema
Kal?ic, Filip,Kolman, Viktor,Ajani, Haresh,Zídek, Zdeněk,Janeba, Zlatko
supporting information, p. 1398 - 1407 (2020/06/17)
We report an extensive structure-activity relationship optimization of polysubstituted pyrimidines that led to the discovery of 5-butyl-4-(4-benzyloxyphenyl)-6-phenylpyrimidin-2-amine, and its difluorinated analogue. These compounds are sub-micromolar inh
Synthesis and AChE inhibitory activity of N-glycosyl benzofuran derivatives
Cao, Zhi-Ling,Liu, Shu-Hao,Liu, Wei-Wei,Liu, Xiu-Jian,Ren, Shu-Ting,Shi, Da-Hua,Wang, Lei,Wang, You-Xian,Wu, Yu-Ran
, p. 162 - 166 (2020/01/28)
Six N-glycosyl benzofuran derivatives were synthesized by the catalysis of organic bases and condensation agents. The benzofuran derivatives were obtained by the reaction of various salicylaldehydes in acetone, and then hydrolyzed to the corresponding carboxylic acids. Finally, the target compounds were synthesized by acylation and the reaction conditions were optimized. The acetylcholinesterase (AChE) inhibitory activity of the desired compounds was tested using Ellman's method. Most of the compounds showed acetylcholinesterase-inhibition activity; N-(2,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)benzofuran-2-carbxamide (5a) showed the best acetylcholinesterase inhibition, with an inhibitory rate of 84%.
Synthetic studies on selective adenosine A2A receptor antagonists: Synthesis and structure-activity relationships of novel benzofuran derivatives
Saku, Osamu,Saki, Mayumi,Kurokawa, Masako,Ikeda, Ken,Takizawa, Takuya,Uesaka, Noriaki
scheme or table, p. 1090 - 1093 (2010/06/15)
A series of benzofuran derivatives were prepared to study their antagonistic activities to the A2A receptor. Replacement of the ester group of the lead compound 1 with phenyl ring improved the PK profile, while modifications of the amide moiety