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Dihydro-alkoxyl-benzyl-oxopyrimidine Derivatives (DABOs) As Non-Nucleoside Reverse Transcriptase Inhibitors: An Update Review (2001-2011)

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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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Keywords: DABOs; DACO analogs; DATNO; HIV-1; HIV-2; NNRTIs; RT; dihydro-alkoxyl-benzyl-oxopyrimidine scaffold; drug resistance mutations; non-nucleoside compounds

Document Type: Research Article

Publication date: 2012-01-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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