The aim of the study is to identify a novel furan-based chalcone derivative as potent inhibitor against the H37Rv strain The pharmacokinetic characteristics, toxicity tests, molecular modeling, chemical synthesis and minimum inhibitory concentration (MIC; IC) were carried out to evaluate the antitubercular potential of the synthesized furan-based chalcone analogues against H37Rv. Among the ten target compounds synthesized, DF02, DF05 and DF07 had MIC values of 1.6 μg/ml equivalent to isoniazid and DF10 showed MIC values of 3.25 μg/ml which is equipotent to pyrazinamide. All the other compounds had optimal concentrations 6.25-100 μg/ml against the H37Rv strain. Compounds DF02 and DF10 were further evaluated for cytotoxicity assay performed using HeLa cell lines.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.4155/fmc-2023-0110 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Furan-based Chalcone Annihilates the Multi-Drug-Resistant Pseudomonas aeruginosa and Protects Zebra Fish Against its Infection.
J Microbiol
February 2024
Toxicology and Pharmacology Laboratory, Department of Biotechnology, Faculty of Science and Humanities, SRM Institute of Science and Technology, Kattankulathur, Chengalpattu District, Chennai, Tamil Nadu, 603203, India.
The emergence of carbapenem-resistant Pseudomonas aeruginosa, a multi-drug-resistant bacteria, is becoming a serious public health concern. This bacterium infects immunocompromised patients and has a high fatality rate. Both naturally and synthetically produced chalcones are known to have a wide array of biological activities.
View Article and Find Full Text PDFSynthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents: , cytotoxicity assessment and .
Future Med Chem
September 2023
Dr APJ Kalam Research Lab, Department of Pharmaceutical Chemistry, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chengalpattu, Tamil Nadu, 603 203, India.
The aim of the study is to identify a novel furan-based chalcone derivative as potent inhibitor against the H37Rv strain The pharmacokinetic characteristics, toxicity tests, molecular modeling, chemical synthesis and minimum inhibitory concentration (MIC; IC) were carried out to evaluate the antitubercular potential of the synthesized furan-based chalcone analogues against H37Rv. Among the ten target compounds synthesized, DF02, DF05 and DF07 had MIC values of 1.6 μg/ml equivalent to isoniazid and DF10 showed MIC values of 3.
View Article and Find Full Text PDFFuran based synthetic chalcone derivative functions against gut inflammation and oxidative stress demonstrated in in-vivo zebrafish model.
Eur J Pharmacol
October 2023
Toxicology and Pharmacology Laboratory, Department of Biotechnology, Faculty of Science and Humanities, SRM Institute of Science and Technology, Kattankulathur, 603203, Chengalpattu District, Tamil Nadu, India. Electronic address:
Inflammatory Bowel Disease (IBD) is a group of persistent intestinal illnesses resulting from bowel inflammation unrelated to infection. The prevalence of IBD is rising in industrialized countries, increasing healthcare costs. Whether naturally occurring or synthetic, chalcones possess a broad range of biological properties, including anti-inflammatory, anti-microbial, and antioxidant effects.
View Article and Find Full Text PDFPharmacophore Modeling, 3D-QSAR and Molecular Docking of Furanochalcones as Inhibitors of Monoamine Oxidase-B.
Cent Nerv Syst Agents Med Chem
February 2017
Division of Drug Design and Medicinal Chemistry Research Lab., Department of Pharmaceutical Chemistry, Grace College of Pharmacy, Palakkad, Kerala, India.
Monoamine oxidase B inhibitors are of particular importance in the treatment of neurodegenerative disorders such as Alzheimer's and Parkinson's disease. Herein described is pharmacophore generation and atom-based 3D-QSAR analysis of previously reported furan based MAO-B inhibitors in order to get insight into their structural requirements responsible for high affinity. The best pharmacophore model generated with the five-point hypotheses of ADHRR: hydrogen bond acceptor (A), hydrogen bond donor (D), hydrophobic (H) and two aromatic rings (R1 & R2).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!