Chemical Biology and Drug Design p. 426 - 433 (2012)
Update date:2022-08-03
Topics:
Zhu, Xiaoyun
Ji, Jianfeng
Huang, Dandan
Zhu, Yan
Tang, Chunlei
Yang, Xuan
Qian, Hai
Huang, Wenlong
Chemical-based common feature pharmacophore modelling of Niemann Pick C1 Like 1 inhibitors was performed to provide some insights on the important pharmacophore features essential for Niemann Pick C1 Like 1 inhibition using Discovery Studio V2.5. After in-house database screening, a new series of substituted oxazolidinones, selected from the top ranked hits, have been synthesized and evaluated as novel cholesterol absorption inhibitors. All compounds demonstrated effect of different degrees in lowering the total cholesterol in serum, especially compounds 1a, 2a and 2d, the potency of which was comparable to that of ezetimibe. It was also found that 1a, 1d and 2d could raise high-density lipoprotein cholesterol levels markedly. Interestingly, compounds 2a-2f appeared to have the moderate potential to lower triglyceride levels, which were superior to that of normal cholesterol absorption inhibitors including ezetimibe. Two classes of novel substituted oxazolidinones were identified by virtual screening as the candidates of cholesterol absorption inhibitors to treat coronary artery disease. All compounds demonstrated effect of different degrees in lowering the total cholesterol in serum. Interestingly, compounds 2a-2f appeared to have the moderate potential to lower triglyceride levels, which were superior to that of normal cholesterol absorption inhibitors including ezetimibe.
View Morewebsite:http://www.finerchem.com
Contact:+86-531-88989536
Address:New Material Industry Park, Jinan Ciyt, China
HAINAN JINYING IMPORT AND EXPORT CO. LTD
Contact:+86-898-32875423
Address:A SECTION 19TH FL, TIMES SQUARE, NO.2 GUO MAO AVENUE HAIKOU, HAINAN, P. R. OF CHINA
Beijing Merson Pharmaceutical Co., Ltd
Contact:0086-10-80484934 0086-10-80484574/
Address:2nd Floor , No. 2 Building , No. 14 Houshayu Duan, Jingmi Road ,Shunyi District , Beijing 101318, P.R.China
Zibo Ocean International Trade Co.,Ltd(expird)
Contact:+86 533 5160706
Address:1117, Hongtai Bld., Songling rd, Zichuan,Zibo,Shandong,China
Lianyungang Ningkang Chemical Co., Ltd
Contact:.+86-518-88588008
Address:http://www.chemnk.com
Doi:10.1039/c2ob25771h
(2012)Doi:10.1016/0022-328X(91)86419-Q
(1991)Doi:10.1016/j.inoche.2012.05.013
(2012)Doi:10.1080/00958972.2012.700053
(2012)Doi:10.1021/co300068a
(2012)Doi:10.1002/ardp.201300051
(2013)