Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
PMID: 14971897
2004
Journal of medicinal chemistry
Abstract: They were particularly potent against NNRTI-resistant viruses containing Y181C-, K103N-, and K103N-based double mutations, which account for a significant proportion of the clinical failure of the three currently marketed NNRTIs.
Synthesis of 6-arylvinyl analogues of the HIV drugs SJ-3366 and Emivirine.
Abstract: The most active compounds 1-ethoxymethyl, 1-(2-propynyloxymethyl), and 1-(2-methyl-3-phenylallyloxymethyl) substituted 6-[1-(3,5-dimethylphenyl)vinyl]-5-ethyl-1H-pyrimidine-2,4-dione (5b, 16, and 18) showed activities against HIV-1 wild type in the range of Efavirenz, and moderate activities against Y181C and Y181C+K103N mutant strains were also observed.
Structural and energetic analyses of the effects of the K103N mutation of HIV-1 reverse transcriptase on efavirenz analogues.
PMID: 15084137
2004
Journal of medicinal chemistry
Abstract: The effect of the K103N mutation of HIV-1 reverse transcriptase (RT) on the activity of efavirenz analogues was studied via Monte Carlo/free energy perturbation calculations.
Abstract: The relative fold resistance energies indicate that efavirenz binds to K103N RT in a manner similar to the wild-type enzyme.
Characterization of a subtype D human immunodeficiency virus type 1 isolate that was obtained from an untreated individual and that is highly resistant to nonnucleoside reverse transcriptase inhibitors.
Abstract: D14-UG did not contain the classic amino acid substitutions conferring NNRTI resistance (e.g., Y181C, K103N, and G190A) but did have some putative sites associated with drug resistance, I135L, T139V, and V245T.
Effect of stereo and regiochemistry towards wild and multidrug resistant HIV-1 virus: viral potency of chiral PETT derivatives.
Abstract: The lead compounds for the respective groups were further tested against A17 (NNRTI-resistant, Y181C mutant RT), and A17Var (NNI-resistant Y181C +/- K103N mutant RT) as well as multidrug resistant viral strains.
Detection of HIV-1 antiretroviral resistance from patients with persistently low but detectable viraemia.
PMID: 15158587
2004
Journal of virological methods
Abstract: Multiple sequencing of samples with low viral load did not result in detection of additional mutations, although, in one sample the K103N mutation was detected in 3/6 replicates while wild-type was detected in 2/6 and a mixture of wild-type/mutant in 1/6.
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
PMID: 15239667
2004
Journal of medicinal chemistry
Abstract: In cell-based assays, the new derivatives showed activities against HIV-1 wild type and NNRTI-resistant mutants [Y181C, K103N-Y181C, and triple mutant (K103R, V179D, P225H) highly resistant to efavirenz] superior to that of the parent indole derivative 1.
Comparison of nevirapine (NVP) resistance in Ugandan women 7 days vs. 6-8 weeks after single-dose nvp prophylaxis: HIVNET 012.
PMID: 15242535
2004
AIDS research and human retroviruses
Abstract: Y181C was the most common NVPR mutation detected at 7 days, whereas K103N was the most common NVPR mutation detected at 6-8 weeks.
Abstract: In contrast, the K103N mutation emerges more slowly, but often remains detectable 6-8 weeks after NVP.
Effect of stereochemistry on the anti-HIV activity of chiral thiourea compounds.
Abstract: The lead compounds in the respective groups were further tested against the NNRTI-resistant HIV strains, A17 (Y181C mutant), and A17Var (Y181C+K103N mutant) and RT MDR (V106N).
Intrapartum exposure to nevirapine and subsequent maternal responses to nevirapine-based antiretroviral therapy.
PMID: 15247339
2004
The New England journal of medicine
Abstract: Resistance mutations to nonnucleoside reverse-transcriptase inhibitors were detectable in blood samples obtained 10 days post partum from 32 percent of the women who had received intrapartum nevirapine; the most frequent mutations were K103N, G190A, and Y181C.
HIV mutation literature information.
PMID: 
2004
Journal of medicinal chemistry
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