N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase
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چکیده
منابع مشابه
Potent Nonnucleoside Reverse Transcriptase Inhibitors Target HIV-1 Gag-Pol
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) target HIV-1 reverse transcriptase (RT) by binding to a pocket in RT that is close to, but distinct, from the DNA polymerase active site and prevent the synthesis of viral cDNA. NNRTIs, in particular, those that are potent inhibitors of RT polymerase activity, can also act as chemical enhancers of the enzyme's inter-subunit interactions. H...
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1-alkoxymethyl-5-alkyl-6-naphthylmethyl uracils, which are novel 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) analogues, were synthesized for evaluation as selective and potent nonnucleoside human immunodeficiency virus (HIV)-1 reverse transcriptase inhibitors. The anti-HIV-1 activity of these compounds was assayed in vitro using HIV-1 infected MT-4 and CEM bioassays. The EC50, CC50...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2013
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2012.12.027