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

Journal

CURRENT MEDICINAL CHEMISTRY
Volume 19, Issue 2, Pages 152-162

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986712803414169

Keywords

DABOs; drug resistance mutations; HIV-1; HIV-2; NNRTIs; RT

Funding

  1. National Natural Science Foundation of China [20872018, 81172918]

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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 structure-activity relationship studies of DABO derivatives and provides new clues for the design of new DABO congeners.

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