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

作者：Yang Shiqiong; Chen Fen Er^*; De Clercq Erik

来源：Current Medicinal Chemistry, 2012, 19(2): 152-162.

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

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.

• 出版日期2012-1
• 单位复旦大学; 河北医科大学