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

Author(s): Shiqiong Yang, Fen-Er Chen, Erik De Clercq

Journal Name: Current Medicinal Chemistry

Volume 19 , Issue 2 , 2012

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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.

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

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Article Details

Year: 2012
Page: [152 - 162]
Pages: 11
DOI: 10.2174/092986712803414169
Price: $65

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