期刊论文详细信息
Journal of The Chilean Chemical Society | |
SYNTHESIS AND EVALUATION OF 5-(6-METHOXYNAPHTHALEN-2-YL)-1-ARYL-1-(4-(TRIFLUOROMETHYL)PHENYLAMINO)PENTAN-3-ONE AS POTENTIAL ANTIDIABETIC AGENTS | |
Fei, YE1  FANG, YAN JU1  LI, FAN2  YAN, HAN HAI2  GUANG-MING, ZHOU2  DA-CHENG, YANG2  JIN, XU2  | |
[1]Drug Screening Center, Chengdu, China | |
[2]Southwest University, Chongqing, China | |
关键词: Diabetes Mellitus; PPRE; α; -; Glucosidase; PTP 1B; ketones; Mannich base; | |
DOI : 10.4067/S0717-97072011000400023 | |
学科分类:化学(综合) | |
来源: Sociedad Chilena de Quimica | |
【 摘 要 】
We wish to report a set of seventeenketones bearing nabumetone and trifluoro- methylaniline(TFMA) moieties. Synthesized via direct Mannich reaction in a solution of ethanol- chloroform catalyzed by concentrated hydrochloric acid, the chemical structures of these compounds were characterized by IR, 1H NMR, 13C NMR, ESI MS and HR MS. Studies on their antidiabetic activities revealed that all title compounds possessed moderate α-glucosidase inhibitory activities and protein tyrosine phosphatase 1B (PTP 1B) inhibitory activities. Among them, a few compounds also exhibit considerable peroxisome proliferator-activated receptor response element (PPRE) agonist activity, in particular the relative PPRE agonist activity of compounds 1r and 1l reached 54.02% and 57.60%, respectively. These results represent significant examples of new molecular type for antidiabetic agents that merit further evaluation.【 授权许可】
Unknown
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