ArticleMolecules (Basel, Switzerland)2015
Antimycobacterial and anti-inflammatory activities of substituted chalcones focusing on an anti-tuberculosis dual treatment approach.
Article in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 59 citations in OpenAlex.
- Antimycobacterial Activity and Nitric Oxide Production Inhibition of Antarctic Seaweeds.ACS omega · 2026Article
- Bioactive Natural and Synthetic Chalcones: Brazil as a Research Powerhouse in Discovery and Innovation.ChemMedChem · 2026Review
- Intracellular and Extracellular Efficacy of Homoisoflavone Derivatives Against Mycobacterium Tuberculosis: Progress Toward Novel Antitubercular Agents.ChemMedChem · 2025Article
- Elucidating molecular mechanism and chemical space of chalcones through biological networks and machine learning approaches.Computational and structural biotechnology journal · 2024Article
- Advances in Aβ imaging probes: a comprehensive study of radiolabelled 1,3-diaryl-2-propen-1-ones for Alzheimer's disease: a review.RSC advances · 2023Review
- Exploring biogenic chalcones as DprE1 inhibitors for antitubercular activity via in silico approach.Journal of molecular modeling · 2023Article
- Identification and Characterization of Two Defensins from Capsicum annuum Fruits that Exhibit Antimicrobial Activity.Probiotics and antimicrobial proteins · 2020Article
- Synthesis, Structure and In Vitro Anti-Trypanosomal Activity of Non-Toxic Arylpyrrole-Based Chalcone Derivatives.Molecules (Basel, Switzerland) · 2020Article
- Synthesis, Biological Assessment, and Structure Activity Relationship Studies of New Flavanones Embodying Chromene Moieties.Molecules (Basel, Switzerland) · 2020Article
- Identification of Chalcone Derivatives as Inhibitors ofFrontiers in chemistry · 2020Article
- Microbial transformations of 4'-methylchalcones as an efficient method of obtaining novel alcohol and dihydrochalcone derivatives with antimicrobial activity.RSC advances · 2018Article
- Binding property of HIV p24 and Reverse transcriptase by chalcones from Pongamia pinnata seeds.Bioinformation · 2018Article
- Synthesis andMedChemComm · 2018Article
- Phloretin Exerts Anti-Tuberculosis Activity and Suppresses Lung Inflammation.Molecules (Basel, Switzerland) · 2017Article
- Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.Bioorganic & medicinal chemistry letters · 2016Article
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Tuberculosis (TB) remains a serious public health problem aggravated by the emergence of M. tuberculosis (Mtb) strains resistant to multiple drugs (MDR). Delay in TB treatment, common in the MDR-TB cases, can lead to deleterious life-threatening inflammation in susceptible hyper-reactive individuals, encouraging the discovery of new anti-Mtb drugs and the use of adjunctive therapy based on anti-inflammatory interventions. In this study, a series of forty synthetic chalcones was evaluated in vitro for their anti-inflammatory and antimycobacterial properties and in silico for pharmacokinetic parameters. Seven compounds strongly inhibited NO and PGE2 production by LPS-stimulated macrophages through the specific inhibition of iNOS and COX-2 expression, respectively, with compounds 4 and 5 standing out in this respect. Four of the seven most active compounds were able to inhibit production of TNF-α and IL-1β. Chalcones that were not toxic to cultured macrophages were tested for antimycobacterial activity. Eight compounds were able to inhibit growth of the M. bovis BCG and Mtb H37Rv strains in bacterial cultures and in infected macrophages. Four of them, including compounds 4 and 5, were active against a hypervirulent clinical Mtb isolate as well. In silico analysis of ADMET properties showed that the evaluated chalcones displayed satisfactory pharmacokinetic parameters. In conclusion, the obtained data demonstrate that at least two of the studied chalcones, compounds 4 and 5, are promising antimycobacterial and anti-inflammatory agents, especially focusing on an anti-tuberculosis dual treatment approach.
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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.