Abstract
Numerous structurally different non-nucleoside compounds have been evaluated for their inhibitory effects against HIV replication, in which DABO derivatives, bearing the dihydro-alkoxyl-benzyl-oxopyrimidine scaffold, have been identified as a particular class of non-nucleoside reverse transcriptase inhibitors (NNRTIs). The S-DABO, NH-DABO, -N-DABO, DATNO and DACO analogs represent various structural chemical modifications of the substituents on C2, C6 and C5 of the pyrimidine ring to obtain potentially higher potency and lower cytotoxicity. This review article describes the recent progress of the chemical modifications and structureactivity relationship studies of DABO derivatives and provides new clues for the design of new DABO congeners.
Keywords: DABOs, drug resistance mutations, HIV-1, HIV-2, NNRTIs, RT, non-nucleoside compounds, dihydro-alkoxyl-benzyl-oxopyrimidine scaffold, DATNO, DACO analogs
Current Medicinal Chemistry
Title: Dihydro-alkoxyl-benzyl-oxopyrimidine Derivatives (DABOs) As Non-Nucleoside Reverse Transcriptase Inhibitors: An Update Review (2001-2011)
Volume: 19 Issue: 2
Author(s): Shiqiong Yang, Fen-Er Chen and Erik De Clercq
Affiliation:
Keywords: DABOs, drug resistance mutations, HIV-1, HIV-2, NNRTIs, RT, non-nucleoside compounds, dihydro-alkoxyl-benzyl-oxopyrimidine scaffold, DATNO, DACO analogs
Abstract: Numerous structurally different non-nucleoside compounds have been evaluated for their inhibitory effects against HIV replication, in which DABO derivatives, bearing the dihydro-alkoxyl-benzyl-oxopyrimidine scaffold, have been identified as a particular class of non-nucleoside reverse transcriptase inhibitors (NNRTIs). The S-DABO, NH-DABO, -N-DABO, DATNO and DACO analogs represent various structural chemical modifications of the substituents on C2, C6 and C5 of the pyrimidine ring to obtain potentially higher potency and lower cytotoxicity. This review article describes the recent progress of the chemical modifications and structureactivity relationship studies of DABO derivatives and provides new clues for the design of new DABO congeners.
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Cite this article as:
Yang Shiqiong, Chen Fen-Er and De Clercq Erik, Dihydro-alkoxyl-benzyl-oxopyrimidine Derivatives (DABOs) As Non-Nucleoside Reverse Transcriptase Inhibitors: An Update Review (2001-2011), Current Medicinal Chemistry 2012; 19 (2) . https://dx.doi.org/10.2174/092986712803414169
DOI https://dx.doi.org/10.2174/092986712803414169 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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