Synthesis and Antiviral Activity of 1,3-Disubstituted Uracils against HIV-1 and HCMV-Reference-Cited by-同舟云学术

Synthesis and Antiviral Activity of 1,3-Disubstituted Uracils against HIV-1 and HCMV

Published:2003-10 Issue:5 Volume:14 Page:271-279
ISSN:2040-2066
Container-title:Antiviral Chemistry and Chemotherapy
language:en
Short-container-title:Antivir Chem Chemother

Author:

Maruyama Tokumi¹²,Kozai Shigetada¹,Yamasaki Tetsuo²,Witvrouw Myriam³,Pannecouque Christophe³,Balzarini Jan³,Snoeck Robert³,Andrei Graciella³,De Clercq Erik³

Affiliation:

1. Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan

2. Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Kyusyu University of Health & Welfare, Nobeoka City, Japan

3. Rega Instituut, Katholieke Universiteit Leuven, Leuven, Belgium

Abstract

The development of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) is an efficient strategy for finding new therapeutic agents against human immunodeficiency virus (HIV). A large number of 6-substituted uracil derivatives have been prepared in order to explore new NNRTIs. However, there are few approaches to anti-HIV agents from 1,3-disubstituted uracil derivatives. Therefore, we tried to prepare several 1,3-disubstituted uracils, which were easily obtainable from uracil by preparation under alkali and Mitsunobu conditions, and examined their antiviral activity against HIV-1 and human cytomegalovirus (HCMV). We found that 1-benzyl-3-(3,5-dimethylbenzyl)uracil and 1-cyanomethyl-3-(3,5-dimethylbenzyl)-4-thiouracil showed powerful inhibition against HCMV and HIV-1, respectively.

Publisher

SAGE Publications

Link

http://journals.sagepub.com/doi/pdf/10.1177/095632020301400506

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