Journal of Medicinal Chemistry p. 1685 - 1701 (1992)
Update date:2022-09-26
Topics:
Thompson
Fitzgerald
Holloway
Emini
Darke
McKeever
Schleif
Quintero
Zugay
Tucker
Schwering
Homnick
Nunberg
Springer
Huff
By tethering of a polar hydrophilic group to the P1 or P1' substituent of a Phe-based hydroxyethylene isostere, the antiviral potency of a series of HIV protease inhibitors was improved. The optimum enhancement of anti-HIV activity was observed with the 4-morpholinylethoxy substituent. The substituent effect is consistent with a model derived from inhibitor docked in the crystal structure of the native enzyme. An X-ray crystal structure of the inhibited enzyme determined to 2.25 A verifies the modeling predictions.
View Morewebsite:http://www.simagchem.com
Contact:+86-592-2680277
Address:21/F Hualong Office Building,No.6 Hubin East Road, Xiamen,China
Changzhou Medi-tech Bioscientific Co., Ltd.
Contact:86-519-83246372
Address:Number 115 Menghedadao Road, Changzhou, Jiangsu, China
Zibo Fuxi'er Chemical Co.,Ltd (Shanxian Fuxi'er Chemical Co.,Ltd)
Contact:+86-533-2091422
Address:Eastern 4 on the 3th Road ,Liangxiang Industrial Park, Zibo city ,Shandong,China
Huaihua Baohua Biotechnology Co.,Ltd
website:http://www.baochengchem.com
Contact:86-519-82698291
Address:HouYang chemical development zone,Jintan,Jiangsu,China (213200)
Lianyungang Ningkang Chemical Co., Ltd
Contact:.+86-518-88588008
Address:http://www.chemnk.com
Doi:10.1016/j.bmc.2007.11.016
(2008)Doi:10.1039/P29950000747
(1995)Doi:10.1002/anie.200704381
(2008)Doi:10.1016/j.bmc.2007.12.022
(2008)Doi:10.3987/COM-07-11262
(2008)Doi:10.1021/jo00366a039
(1986)