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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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

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

Volume 19 , Issue 2 , 2012

Page: [152 - 162] Pages: 11

DOI: 10.2174/092986712803414169

Price: $65


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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