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 MorePurestar Chem Enterprise Co.,Ltd
website:http://www.purestarchem.com
Contact:05722157374
Address:no235.huanchengdong Rd
Jinan Baozhao Pharmaceutical Co., Ltd
Contact:0086-531-86397156 82371858 82371868
Address:Huaneng Road, Jinan, Shandong ,China
Wuhan Soleado Technology Co.,Ltd.
Contact:86-2783341481 18971291927
Address:RM2405 Unit 1 Builing 1, Taiyin Tower, Changqing Road,Wuhan China
ALPHA PHARMACEUTICAL CO，LTD JIANGSU
Contact:+86-527-84829968,+86-527-84829998
Address:suqian city
Shanghai Puda Chemical Co.,Ltd
Contact:+86+571+56565965
Address:10F Haiyue Building,Danfeng Road,Binjiang District,Hangzhou,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)
