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Recent Advances in the DABOs Family as Potent HIV-1 non-Nucleoside Reverse Transcriptase Inhibitors

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HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) bind to an allosteric site on reverse transcriptase (RT) and are a key component of highly active anti-retroviral therapy (HAART) combination regimen for clinical treatment of HIV/AIDS. However, the rapid emergence of drug resistance has limited NNRTIs' clinical option. Therefore, there is an urgent need for the design and development of new and safe NNRTIs that are specifically active against drug-resistant viral strains. DABOs family is one representative of the reported potent HIV-1 NNRTIs, with robust anti-HIV-1 activity against both the wild-type (wt) and drug-resistant isolates carrying multiple RT gene mutations. Three generations of DABO analogues have been studied up to now, i.e.: dihydroalkyloxybenzyloxopyrimidines (O-DABOs), dihydroalkylthiobenzyloxopyrimidines (S-DABOs) and dihydroalkylaminodifluorobenzyloxopyrimidines (N-DABOs), from which many promising DABOs are under developed. The recent research of the DABOs family in antiviral activity, structure activity relationships (SAR), and interaction model with the HIV-1 RT are reviewed in this paper.


Document Type: Research Article


Publication date: June 1, 2011

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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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