Title of article
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases
Author/Authors
Alexandre Gagnon، نويسنده , , Ma’an H. Amad، نويسنده , , Pierre R. Bonneau، نويسنده , , René Coulombe، نويسنده , , Patrick L. DeRoy، نويسنده , , Louise Doyon، نويسنده , , Jianmin Duan، نويسنده , , Michel Garneau، نويسنده , , Ingrid Guse، نويسنده , , Araz Jakalian، نويسنده , , Eric Jolicoeur، نويسنده , , Serge Landry، نويسنده , , Eric Malenfant، نويسنده , , Bruno Simoneau، نويسنده , , Christiane Yoakim، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
4437
To page
4441
Abstract
A series of aryl thiotetrazolylacetanilides were synthesized and found to be potent inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases. The incorporation of an alkynyl fragment on the aniline provided inhibitors with excellent cellular activity and extensive SAR led to the identification of one inhibitor having good oral bioavailability in rats.
Keywords
Molecular modeling , Double mutant reverse transcriptase , Non-nucleoside reverse transcriptase inhibitor (NNRTI) , Thiotetrazoles , Alkynes , SAR , Pharmacokinetics
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798438
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