Bioorganic and Medicinal Chemistry Letters p. 1227 - 1231 (2000)
Update date:2022-07-30
Topics:
Matsumoto, Hikaru
Hamawaki, Tomonori
Ota, Hisashi
Kimura, Tooru
Goto, Toshiyuki
Sano, Kouichi
Hayashi, Yoshio
Kiso, Yoshiaki
We designed and synthesized a new series of prodrug-type anti-HIV agents consisting of a peptidomimetic HIV protease inhibitor conjugated with a nucleoside reverse transcriptase inhibitor in an effort to enhance the antiviral activity. For the conjugation, a series of linkers that conjoin the two different classes of inhibitors have been investigated. Conjugates using a succinyl amino acid linker were shown to release the parent components via the spontaneous imide formation at a faster rate compared to conjugates using a glutaryl amino acid linker, as expected from the energetically favorable cyclization to the five-membered ring. Herein, we report a new 'double-drug' 4b (KNI-1039) with a glutarylglycine linker, which exhibited extremely potent anti-HIV activity compared with that of the individual components. (C) 2000 Elsevier Science Ltd. All rights reserved.
View MoreSHANDONG ZHANHUA YONGHAO PHARMACEUTICAL TECH.CO.,LTD
Contact:+86-576-88685096
Address:GENGJU VILLAGE NORTH ONE KILOMETER,ZHANHUA DISTRICT,BINZHOU CITY,SHANDONG PROVINCE,CHINA.
Shanghai PuYi Chem-Tech Co.,Ltd.
Contact:+86-21-57687505-227
Address:3 Floor, Building 11, No 201 MinYi Road, Songjiang District, Shanghai 201612, China
Chongqing maohuan Chemicals Co., Ltd
website:http://www.bschem.com
Contact:+86 13996103726
Address:Chongqing Nan'an District Tu Town
Tianjin Jingye Fine Chemicals Co., Ltd.
Contact:+86-15722078107; +86-22-26911407
Address:Bohua Fine Chemicals Base of Petrochemical Industry Park, Nanhuan Road, Dagang District, Tianjin, 300271, P. R. China
Contact:+86-633-8332928
Address:No.1,Huanghai Yilu.Rizhao,Shandong
Doi:10.1016/S0040-4039(01)97291-0
(1971)Doi:10.1016/S0968-0896(00)00274-1
(2001)Doi:10.1021/jo010625v
(2002)Doi:10.1002/hlca.19710540620
(1971)Doi:10.1080/10587250008023599
(2000)Doi:10.1016/S0008-6215(00)84946-0
(1971)