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 MoreAnhui Jiatiansen Agrochemical Co.,Ltd
Contact:15366811918
Address:chemical industrial park,xiangyu town,dongzhi county,anhui,china
zhangjiagang bonded areas banggao co;ltd
website:http://www.shunchangchem.com
Contact:0086-13921972933
Address:Dongsha Chemical Zone.Zhangjiagang, Jiangsu Province
Tianjin Ji Ping Jia Chemical Co., Ltd.
Contact:18622448868
Address:tianjin
Qida Chemical Co., Ltd.(expird)
Contact:+86-25-8776 0031
Address:3-2001 Jiaye Int'l Town, 158 Lushan Road,Nanjing, 210019, China
Suzhou Sinosun Imp.&Exp. Corporation
website:http://www.szsinosun.com
Contact:+86-512-63488895,63488616
Address:No.758 East Jiangling Road Wujiang Economic & Technological Developmenty Zone Jiangsu China
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)