Bioorganic and Medicinal Chemistry Letters p. 597 - 600 (1997)
Update date:2022-09-26
Topics:
Brown, George R.
Foubister, Alan J.
Freeman, Susan
McTaggart, Fergus
Mirrlees, Donald J.
Reid, Alan C.
Smith, Graham J.
Taylor, Melvyn J.
Thomason, Douglas A.
Whittamore, Paul R. O.
Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol 1c, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral ED50 of 1c, for the inhibition of rat cholesterol biosynthesis was 1.3 ± 0.45 mg/kg and for the R-enantiomer 1m, 0.8 ± 0.2 mg/kg, with the corresponding R-carboxylic acid 6a, being 0.9 ± 0.25 mg/kg.
View MoreChengda Pharmaceuticals Co., Ltd.
Contact:+86-573-84601188
Address:hengshan Road 5# in Jiashan, zhejiang
Changzhou Qidi Chemical Co., Ltd
website:http://www.czqdhg.com/
Contact:86-519-83382137
Address:128-1-16# HuaYuan Street,Hutang Town,Wujin District,Changzhou City,P.R.China.
Jinan Jiaquan Chemical Co.,Ltd
Contact:+86-531-62318366
Address:Room 502 of Yidonghuayuan No.601 Huaxin Road Licheng District Jinan China
website:http://www.greenutra.cn
Contact:0086-411-39553357
Address:No. 7-1-1802, Huizhi Garden,Ocean Square,Dalian, 116033, China
NINGBO PANGS CHEM INT’L CO.,LTD.
Contact:+86-574-27666845
Address:FLOOR 21,BUILDING NO.11,XIN TIAN DI,NO.689 SHI JI ROAD,NINGBO CHINA
Doi:10.1039/jr9490002656
(1949)Doi:10.1021/jm100576z
(2010)Doi:10.1021/ol500225x
(2014)Doi:10.1021/ol403426u
(2014)Doi:10.1002/anie.201503373
(2015)Doi:10.1016/0022-328X(95)05596-H
(1996)
