ArticleChemical biology & drug design2010
Inhibition of HIV-1 replication by isoxazolidine and isoxazole sulfonamides.
Article in Chemical biology & drug design, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
17 citing papers in PubMed, 97 citations in OpenAlex.
- Nitrone chemistry: a versatile gateway to diverse heterocycles.RSC advances · 2025Review
- Acid-catalysed rearrangement of acyl groups: synthesis of β-d-gluco aminocyclopentitols and carbanucleoside derivatives.RSC advances · 2025Article
- Rational Drug Discovery for Isoxazole Based VEGFR2 Inhibition.Current drug discovery technologies · 2025Article
- Synthesis of novel sulphamethoxazole derivatives and exploration of their anticancer and antimicrobial properties.PloS one · 2023Article
- Fruit juice mediated multicomponent reaction for the synthesis of substituted isoxazoles and their in vitro bio-evaluation.Scientific reports · 2021Article
- Past and Current Progress in the Development of Antiviral/Antimicrobial Polymer Coating towards COVID-19 Prevention: A Review.Polymers · 2021Review
- Triazolo Based-Thiadiazole Derivatives. Synthesis, Biological Evaluation and Molecular Docking Studies.Antibiotics (Basel, Switzerland) · 2021Article
- Inhibitory Activity of Pyrroloisoxazolidine Derivatives againstBioMed research international · 2021Article
- Novel Isoxazolidine and γ-Lactam Analogues of Homonucleosides.Molecules (Basel, Switzerland) · 2019Article
- Pharmaceutical and medicinal significance of sulfur (SEuropean journal of medicinal chemistry · 2019Review
- Crystal structure of (1S,2S,2'R,3a'S,5R)-2'-[(5-bromo-1H-indol-3-yl)meth-yl]-2-isopropyl-5,5'-dimethyl-dihydro-2'H-spiro-[cyclo-hexane-1,6'-imidazo[1,5-b]isoxazol]-4'(5'H)-one.Acta crystallographica. Section E, Crystallographic communications · 2016Article
- Crystal structure of 2-isopropyl-5,7'-dimethyl-1',3',3a',6',8a',8b'-hexa-hydro-spiro-[cyclo-hexane-1,6'-furo[3,4-d]imidazo[1,5-b]isoxazol]-8'(7'H)-one.Acta crystallographica. Section E, Crystallographic communications · 2016Article
- HIV-1 capsid is involved in post-nuclear entry steps.Retrovirology · 2016Article
- 4-(1H-Pyrazol-1-yl) benzenesulfonamide derivatives: identifying new active antileishmanial structures for use against a neglected disease.Molecules (Basel, Switzerland) · 2012Article
- Stereoselective isoxazolidine synthesis via copper-catalyzed alkene aminooxygenation.The Journal of organic chemistry · 2012Article
- 3-(3-Chloro-phen-yl)-1-methyl-3,3a,4,9b-tetra-hydro-1H-chromeno[4,3-c]isoxazole-3a-carbonitrile.Acta crystallographica. Section E, Structure reports online · 2011Article
- Gyrase B inhibitor impairs HIV-1 replication by targeting Hsp90 and the capsid protein.The Journal of biological chemistry · 2010Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Targeting host factors is a complementary strategy for the development of new antiviral drugs. We screened a library of isoxazolidine and isoxazole sulfonamides and found four compounds that inhibited HIV-1 infection in human CD4+ lymphocytic T cells with no toxicity at IC(90) concentrations. Structure-activity relationship showed that benzyl sulfonamides and a halo-substituted aromatic ring on the heterocycle scaffold were critical for antiretroviral activity. The size and position of the incorporated halogen had a marked effect on the antiretroviral activity. The sulfonamide derivatives had no significant effect on HIV-1 entry, reverse transcription and integration but impaired a step necessary for activation of viral gene expression. This step was Tat-independent, strongly suggesting that the target is a cell factor. A virus partially resistant to the least potent compounds could be selected but could not be propagated in the long term, consistent with the possibility that HIV-1 may be less likely to develop resistance against drugs targeting some host factors. Here, we provide evidence that novel synthetic methods can be applied to develop small molecules with antiretroviral activity that target host factors important for HIV-1 replication.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.