ArticleDaru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences2015
Synthesis, HIV-1 RT inhibitory, antibacterial, antifungal and binding mode studies of some novel N-substituted 5-benzylidine-2,4-thiazolidinediones.
Article in Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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11 citing papers in PubMed.
- Medicinal Chemistry Aspects of Thiazole and Thiazolidine Derivatives as Fundamental Building Blocks to Design New NNRTIs Against HIV-1 Reverse Transcriptase.ChemMedChem · 2026Review
- Exploration of Glitazone/Thiazolidinedione Derivatives: Molecular Design and Therapeutic Potential.Bioengineering (Basel, Switzerland) · 2025Review
- An Insight into Rational Drug Design: The Development of In-House Azole Compounds with Antimicrobial Activity.Antibiotics (Basel, Switzerland) · 2024Review
- Synthetic Strategies of Thiazolidine-2,4-dione Derivatives for the Development of New Anti-diabetic Agents: Compressive Review.Current topics in medicinal chemistry · 2024Review
- Novel Thiazolidine-2,4-dione-trimethoxybenzene-thiazole Hybrids as Human Topoisomerases Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics - synthesis and properties.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Thiazolidin-2,4-Dione Scaffold: An Insight into Recent Advances as Antimicrobial, Antioxidant, and Hypoglycemic Agents.Molecules (Basel, Switzerland) · 2022Review
- Synthesis, biological evaluation and in-silico ADME studies of novel series of thiazolidin-2,4-dione derivatives as antimicrobial, antioxidant and anticancer agents.BMC chemistry · 2022Article
- Design and synthesis of novel (Z)-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-3-((1-substituted phenyl-1H-1,2,3-triazol-4-yl)methyl)thiazolidine-2,4-diones: a potential cytotoxic scaffolds and their molecular modeling studies.Molecular diversity · 2021Article
- Mechanisms of Candida Resistance to Antimycotics and Promising Ways to Overcome It: The Role of Probiotics.Probiotics and antimicrobial proteins · 2021Review
- Anti-HIV-1 reverse transcriptase property of some edible mushrooms in Asia.Saudi journal of biological sciences · 2021Article
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4 authors.
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Abstract
backgroundStructural modifications of thiazolidinediones at 3rd and 5th position have exhibited significant biological activities. In view of the facts, and based on in silico studies carried out on thiazolidine-2,4-diones as HIV-1- RT inhibitors, a novel series of 2,4-thiazolidinedione analogs have been designed and synthesized.
methodsTitle compounds were prepared by the reported method. Conformations of the structures were assigned on the basis of results of different spectral data. The assay of HIV-1 RT was done as reported by Silprasit et al. Antimicrobial activity was determined by two fold serial dilution method. Docking study was performed for the highest active compounds by using Glide 5.0.
resultsThe newly synthesized compounds were evaluated for their HIV-1 RT inhibitory activity. Among the synthesized compounds, compound 24 showed significant HIV-1 RT inhibitory activity with 73% of inhibition with an IC50 value of 1.31 μM. Compound 10 showed highest activity against all the bacterial strains.A molecular modeling study was carried out in order to investigate the possible interactions of the highest active compounds 24, 10 and 4 with the non nucleoside inhibitory binding pocket(NNIBP) of RT, active site of GlcN-6-P synthase and cytochrome P450 14-α-sterol demethylase from Candida albicans (Candida P450DM) as the target receptors respectively using the Extra Precision (XP) mode of Glide software.
conclusionA series of novel substituted 2-(5-benzylidene-2,4-dioxothiazolidin-3-yl)-N-(phenyl)propanamides (4-31) have been synthesized and evaluated for their HIV-1 RT inhibitory activity, antibacterial and antifungal activities. Some of the compounds have shown significant activity. Molecular docking studies showed very good interaction.
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