ArticleJournal of medicinal chemistry2014
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
What it found
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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.
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Who cites it
23 citing papers in PubMed.
- Flavonoids in treatment of tuberculosis: from molecular mechanisms to structure activity relationships.Molecular biology reports · 2026Review
- 3-(Pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives: synthesis,RSC medicinal chemistry · 2026Article
- Chromones as Photocatalyzed HAT Reagent and Michael Acceptor for Direct C-H Alkylation of 2-Substituted 4-Chromanones.Research (Washington, D.C.) · 2026Article
- Recent Advances in the Third Order Nonlinear Optical Properties of Chalcone Derivatives: a Review.Journal of fluorescence · 2026Review
- Novel Compounds Target Aberrant Calcium Signaling in the Treatment of Relapsed High-Risk Neuroblastoma.International journal of molecular sciences · 2025Article
- Synthesis of Chromene-linked Bis-indole Derivatives as Selective Tumor-associated Carbonic Anhydrase IX Inhibitors.Anti-cancer agents in medicinal chemistry · 2025Article
- Antimicrobial activity and mechanism of anti-MRSA of phloroglucinol derivatives.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024Article
- Antibacterial Effects of Flavonoids and Their Structure-Activity Relationship Study: A Comparative Interpretation.Molecules (Basel, Switzerland) · 2022Review
- Chromanone-A Prerogative Therapeutic Scaffold: An Overview.Arabian journal for science and engineering · 2022Review
- Comprehensive insight into anti-staphylococcal and anti-enterococcal action of brominated and chlorinated pyrazine-based chalcones.Frontiers in microbiology · 2022Article
- Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors.Frontiers in chemistry · 2022Article
- Rigid 3D-spiro chromanone as a crux for efficient antimicrobial agents: synthesis, biological and computational evaluation.RSC advances · 2021Article
- Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents.Molecules (Basel, Switzerland) · 2020Article
- Gut Bacteria of Water Monitor Lizard (Antibiotics (Basel, Switzerland) · 2019Article
- Synthesis and In Vitro Antibacterial Activity of Quaternized 10-Methoxycanthin-6-one Derivatives.Molecules (Basel, Switzerland) · 2019Article
- Pharmacophore Modeling, Synthesis, and Antibacterial Evaluation of Chalcones and Derivatives.ACS omega · 2018Article
- Synthesis of 8',11'-dihydrospiro[cyclohexane-1,2'-oxepino[2,3-RSC advances · 2018Article
- Biocatalytic access to diverse prenylflavonoids by combining a regiospecificActa pharmaceutica Sinica. B · 2018Article
- New Chromane-Based Derivatives as Inhibitors ofMolecules (Basel, Switzerland) · 2018Article
- Bis-spirochromanones as potent inhibitors of Mycobacterium tuberculosis: synthesis and biological evaluation.Molecular diversity · 2017Article
Corrections and comments
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Authors and funding
14 authors.
Funding
Abstract
On the basis of recently reported abyssinone II and olympicin A, a series of chemically modified flavonoid phytochemicals were synthesized and evaluated against Mycobacterium tuberculosis and a panel of Gram-positive and -negative bacterial pathogens. Some of the synthesized compounds exhibited good antibacterial activities against Gram-positive pathogens including methicillin resistant Staphylococcus aureus with minimum inhibitory concentration as low as 0.39 μg/mL. SAR analysis revealed that the 2-hydrophobic substituent and the 4-hydrogen bond donor/acceptor of the 4-chromanone scaffold together with the hydroxy groups at 5- and 7-positions enhanced antibacterial activities; the 2',4'-dihydroxylated A ring and the lipophilic substituted B ring of chalcone derivatives were pharmacophoric elements for antibacterial activities. Mode of action studies performed on selected compounds revealed that they dissipated the bacterial membrane potential, resulting in the inhibition of macromolecular biosynthesis; further studies showed that selected compounds inhibited DNA topoisomerase IV, suggesting complex mechanisms of actions for compounds in this series.
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