PLoS ONE (2017)
Update date:2022-08-03
Topics:
Kwong, Huey Chong
Kumar, C. S. Chidan
Mah, Siau Hui
Chia, Tze Shyang
Quah, Ching Kheng
Loh, Zi Han
Chandraju, Siddegowda
Lim, Gin Keat
Biphenyl-based compounds are clinically important for the treatments of hypertension and inflammatory, while many more are under development for pharmaceutical uses. In the present study, a series of 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl benzoates, 2(a-q), and 2-([1,1'- biphenyl]-4-yl)-2-oxoethyl pyridinecarboxylate, 2(r-s) were synthesized by reacting 1-([1,1'- biphenyl]-4-yl)-2-bromoethan-1-one with various carboxylic acids using potassium carbonate in dimethylformamide at ambient temperature. Single-crystal X-ray diffraction studies revealed a more closely packed crystal structure can be produced by introduction of biphenyl moiety. Five of the compounds among the reported series exhibited significant antityrosinase activities, in which 2p, 2r and 2s displayed good inhibitions which are comparable to standard inhibitor kojic acid at concentrations of 100 and 250 μg/mL. The inhibitory effects of these active compounds were further confirmed by computational molecular docking studies and the results revealed the primary binding site is active-site entrance instead of inner copper binding site which acted as the secondary binding site.
View MoreShanghai Yuanye Bio-Technology Co., Ltd.
website:http://www.shyuanye.com
Contact:+86-21-61845781
Address:Building 6, No. 465, Changta Road,Songjiang District,Shanghai,China
TAIXING BEST NEW MATERIALS CO., LTD
Contact:0523-87998158;
Address:No.18 Zhonggang Road,Taixing City ,Jiangsu , China
NINGBO YINZHOU PRECISE COLOR CO.,LTD.
Contact:86-574-88139809 86-574-83033159
Address:Qiming Road,Yinzhou,Ningbo,China
Wuhan Chemwish Technology Co., Ltd
website:http://www.chemwish.com/
Contact:+86-27-67849912
Address:Room 1311, Unit 2, Block1, Innovation Road East Lake High-tech Development Zone Wuhan, Hubei,P.R. China
Chongqing maohuan Chemicals Co., Ltd
website:http://www.bschem.com
Contact:+86 13996103726
Address:Chongqing Nan'an District Tu Town
Doi:10.1055/s-0029-1216871
(2009)Doi:10.1002/chem.201800316
(2018)Doi:10.1002/jhet.5570370622
(2000)Doi:10.1039/C39760000321
(1976)Doi:10.1023/A:1005464326573
(2000)Doi:10.1021/ic50102a032
(1971)