DB-02, a C-6-cyclohexylmethyl substituted pyrimidinone HIV-1 reverse transcriptase inhibitor with nanomolar activity, displays an improved sensitivity against K103N or Y181C than S-DABOs

scientific article (publication date: 2013)

DB-02, a C-6-cyclohexylmethyl substituted pyrimidinone HIV-1 reverse transcriptase inhibitor with nanomolar activity, displays an improved sensitivity against K103N or Y181C than S-DABOs is …
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scholarly articleQ13442814

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P819ADS bibcode2013PLoSO...881489Z
P356DOI10.1371/JOURNAL.PONE.0081489
P932PMC publication ID3839930
P698PubMed publication ID24282600
P5875ResearchGate publication ID258956326

P2093author name stringYong-Tang Zheng
Liu-Meng Yang
Rong-Hua Luo
Xing-Jie Zhang
Rui-Rui Wang
Yue-Ping Wang
Yan-Ping He
Li-He Lu
Christopher Cong Lai
P2860cites workDiscovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutantsQ39895940
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Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activityQ40342543
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Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptaseQ40790038
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO seriesQ41110624
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.Q41309346
TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experimentsQ42033549
Near full-length genomic characterization of a novel HIV type 1 subtype B/C recombinant strain from Yunnan, ChinaQ46182378
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profileQ46481272
Roles of Conformational and Positional Adaptability in Structure-Based Design of TMC125-R165335 (Etravirine) and Related Non-nucleoside Reverse Transcriptase Inhibitors That Are Highly Potent and Effective against Wild-Type and Drug-Resistant HIV-1 VQ57480046
Synthesis, Biological Activity, and ADME Properties of Novel S-DABOs/N-DABOs as HIV Reverse Transcriptase InhibitorsQ60197481
[In vitro selection and identification of HIV strain which is resistance to two new HIV-1 nonnucleoside reverse transcriptase inhibitors]Q83476569
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivativesQ28370647
A comprehensive mapping of HIV-1 genotypes in various risk groups and regions across China based on a nationwide molecular epidemiologic surveyQ28484277
A semiempirical free energy force field with charge-based desolvationQ29614316
Drug combination studies and their synergy quantification using the Chou-Talalay methodQ29617422
Lower in vivo mutation rate of human immunodeficiency virus type 1 than that predicted from the fidelity of purified reverse transcriptaseQ29619994
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.Q31138625
Low frequency nonnucleoside reverse-transcriptase inhibitor-resistant variants contribute to failure of efavirenz-containing regimens in treatment- experienced patientsQ33714377
Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agentsQ33782941
Development of drug resistance in patients receiving combinations of zidovudine, didanosine and nevirapineQ33953120
Anti-human immunodeficiency virus type 1 activity of novel 6-substituted 1-benzyl-3-(3,5-dimethylbenzyl)uracil derivativesQ34145448
Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.Q34910804
Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: a review of the last 20 years (1989-2009).Q35005228
Human immunodeficiency virus reverse transcriptase: 25 years of research, drug discovery, and promiseQ36435971
Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIV reverse transcriptaseQ37099790
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Dihydro-alkoxyl-benzyl-oxopyrimidine derivatives (DABOs) as non-nucleoside reverse transcriptase inhibitors: an update review (2001-2011).Q37982772
The development of HEPT-type HIV non-nucleoside reverse transcriptase inhibitors and its implications for DABO familyQ38012497
Molecular basis of human immunodeficiency virus type 1 drug resistance: overview and recent developments.Q38081000
Assessing adherence to antiretroviral therapy in randomized HIV clinical trials: a review of currently used methodsQ38086335
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitorsQ39522504
The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3, 4-dihydropyrimidin-4 (3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in vitro.Q39586664
Synthesis and biological evaluation of 6-substituted 5-alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as potent HIV-1 NNRTIsQ39591934
F18, a novel small-molecule nonnucleoside reverse transcriptase inhibitor, inhibits HIV-1 replication using distinct binding motifs as demonstrated by resistance selection and docking analysis.Q39692280
Sifuvirtide, a potent HIV fusion inhibitor peptide.Q39872319
P275copyright licenseCreative Commons Attribution 3.0 UnportedQ14947546
P6216copyright statuscopyrightedQ50423863
P433issue11
P407language of work or nameEnglishQ1860
P304page(s)e81489
P577publication date2013-01-01
P1433published inPLOS OneQ564954
P1476titleDB-02, a C-6-cyclohexylmethyl substituted pyrimidinone HIV-1 reverse transcriptase inhibitor with nanomolar activity, displays an improved sensitivity against K103N or Y181C than S-DABOs
P478volume8

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cites work (P2860)
Q28542490Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in vitro
Q92284526Clerodane diterpenoids with potential anti-inflammatory activity from the leaves and twigs of Callicarpa cathayana
Q38260066Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2011-2014).
Q50129893SJP-L-5 inhibits HIV-1 polypurine tract primed plus-strand DNA elongation, indicating viral DNA synthesis initiation at multiple sites under drug pressure.
Q35859394SJP-L-5, a novel small-molecule compound, inhibits HIV-1 infection by blocking viral DNA nuclear entry
Q38746848Synthesis and Anti-HIV-1 Activity Evaluation for Novel 3a,6a-Dihydro-1H-pyrrolo[3,4-c]pyrazole-4,6-dione Derivatives.
Q90094399Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones as potential HIV-1 inhibitors

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