Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.

doi:10.1016/j.bmc.2010.03.007

Paper

DOI: 10.1016/j.bmc.2010.03.007

Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.

Published Apr 1, 2010 · Xiao-qing Feng, Zhao‐sen Zeng, Yong‐Hong Liang

Bioorganic & medicinal chemistry

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Abstract

Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.

In Vitro Study

Study Snapshot

Novel diarylpyrimidine analogues show moderate to excellent activity against HIV, with 4-(4-((Hydroxyimino)-3-methoxyphenyl)methyl)pyrimidin-2-ylamino)benzonitrile being the most active compound.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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References

DOI: 10.1016/j.bmcl.2009.07.080

Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Diarylpyridine derivatives show potential as a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors, active against both wild-type and drug-resistant strains.

2009·25citations·Xing-tao Tian et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1002/cmdc.200900212

Design, Synthesis, and SAR of Naphthyl‐Substituted Diarylpyrimidines as Non‐Nucleoside Inhibitors of HIV‐1 Reverse Transcriptase

Naphthyl-substituted diarylpyrimidines show strong activity against HIV-1 reverse transcriptase, with the most active compound showing a selectivity index of over 180 000 against wild-type HIV-1.

2009·36citations·Yong‐Hong Liang et al.·ChemMedChem

ChemMedChem

DOI: 10.1016/j.bmc.2008.01.039

Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones show moderate to potent anti-HIV-1 activity, with the 6-(3,5-dimethylbenzyl) analogue 5p showing the most promising activity

2008·14citations·Yueping Wang et al.·Bioorganic & medicinal chemistry

Bioorganic & medicinal chemistry

DOI: 10.1016/J.EJMECH.2006.11.014

Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.

Novel diarylpyrimidine analogues of TMC278 show high potency against HIV-1 wild-type and mutant strains, with potential for future clinical trials.

2007·67citations·Céline Mordant et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.1021/JM061167R

Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.

Novel S-DABO analogues show potent and selective anti-HIV-1 activity, with two showing unusually high potency and selectivity.

2007·40citations·L. Ji et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

DOI: 10.1021/JM040838N

Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.

New diarylpyrimidine compounds show improved antiviral activity against clinically relevant HIV-1 strains, offering potential for future clinical trials.

2005·110citations·J. Guillemont et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

DOI: 10.1016/J.BMCL.2004.11.063

(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors.

The less lipophilic derivatives 3a-c show the most potent inhibitory activity on human Lp-PLA2, suggesting potential as pharmaceutical agents for treating human Lp-PLA2 deficiency.

2005·23citations·T. Jeong et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1016/J.BMCL.2004.04.008

5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.

Novel S-DABOs show potential as potent anti-HIV agents, with some showing activity against both HIV-1 and HIV-2, and may act differently than classical NNRTIs.

2004·42citations·Yan-ping He et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

Citations

DOI: 10.1016/j.ejmech.2024.116973

Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors (2019-2023).

Diarylpyrimidines and their analogues have evolved from 2019 to 2023, focusing on improving resistance profiles, optimizing pharmacokinetics, and reducing toxicity and side effects.

2024·0citations·Mu-Zi Nie et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.1002/med.21760

Druggability modification strategies of the diarylpyrimidine‐type non‐nucleoside reverse transcriptase inhibitors

Diarylpyrimidine-type NNRTIs show promise in combating HIV resistance, but require druggability modifications to improve antiviral activity, reduce toxicity, and enhance pharmacokinetic properties.

2021·28citations·Li Ding et al.·Medicinal Research Reviews

Medicinal Research Reviews

DOI: 10.1016/j.coph.2020.09.017

Recent discoveries in HIV-1 reverse transcriptase inhibitors.

Recent discoveries in HIV-1 reverse transcriptase inhibitors, including approved drugs and promising candidates, offer promising future direction for controlling AIDS and reducing morbidity and mortality in HIV-infected patients.

2020·34citations·Shuang‐Xi Gu et al.·Current opinion in pharmacology

Current opinion in pharmacology

DOI: 10.1016/j.apsb.2019.11.010

Development of non-nucleoside reverse transcriptase inhibitors (NNRTIs): our past twenty years

In the last 20 years, our medicinal chemistry group has developed several novel NNRTIs using modern medicinal strategies, including structure-based drug design and fragment-based optimization.

2019·87citations·Chunlin Zhuang et al.·Acta Pharmaceutica Sinica. B

Acta Pharmaceutica Sinica. B

DOI: 10.1016/j.ejmech.2019.111603

Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.

The study developed potent HIV-1 NNRTIs with halogen and methyl groups, showing lower cytotoxicity and higher selectivity compared to etravirine.

2019·24citations·Y. Sang et al.·European journal of medicinal chemistry

European journal of medicinal chemistry