Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Discovery of Quinazolone Pyridiniums as Potential Broad-Spectrum Antibacterial Agents.
Molecules
January 2025
Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China.
The overprescription of antibiotics in medicine and agriculture has accelerated the development and spread of antibiotic resistance in bacteria, which severely limits the arsenal available to clinicians for treating bacterial infections. This work discovered a new class of heteroarylcyanovinyl quinazolones and quinazolone pyridiniums to surmount the increasingly severe bacterial resistance. Bioactive assays manifested that the highly active compound exhibited strong inhibition against MRSA and with extremely low MICs of 0.
View Article and Find Full Text PDFDiscovery of novel deoxyvasicinone derivatives with benzenesulfonamide substituents as multifunctional agents against Alzheimer's disease.
Eur J Med Chem
January 2024
The Key Laboratory for Joint Construction of Synthetic Bioprotein of Anhui Province, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Institute of Innovative Drugs, School of Pharmacy, Anhui Medical University, Hefei, China. Electronic address:
A series of deoxyvasicinone derivatives with benzenesulfonamide substituents were designed and synthesized to find a multifunctional anti-Alzheimer's disease (AD) drug. The results of the biological activity evaluation indicated that most compounds demonstrated selective inhibition of acetylcholinesterase (AChE). Among them, g17 exhibited the most potent inhibitory effect on AChE (IC = 0.
View Article and Find Full Text PDFAccommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
Eur J Med Chem
October 2022
School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, 110031, Taiwan. Electronic address:
A fragment recruitment process was conducted to pinpoint a suitable fragment for installation in the HDAC inhibitory template to furnish agents endowed with the potential to treat lung cancer. Resultantly, Ring C expanded deoxyvasicinone was selected as an appropriate surface recognition part that was accommodated in the HDAC three-component model. Delightfully, fused quinazolinone 6 demonstrating a magnificent anticancer profile against KRAS and EGFR mutant lung cancer cell lines (IC = 0.
View Article and Find Full Text PDFDeoxyvasicinone with Anti-Melanogenic Activity from Marine-Derived sp. CNQ-617.
Mar Drugs
February 2022
College of Pharmacy, Ewha Womans University, Seoul 03760, Korea.
The tricyclic quinazoline alkaloid deoxyvasicinone (, ) was isolated from a marine-derived sp. CNQ-617, and its anti-melanogenic effects were investigated. Deoxyvasicinone was shown to decrease the melanin content of B16F10 and MNT-1 cells that have been stimulated by α-melanocyte-stimulating hormone (α-MSH).
View Article and Find Full Text PDFDual targeting of acetylcholinesterase and tau aggregation: Design, synthesis and evaluation of multifunctional deoxyvasicinone analogues for Alzheimer's disease.
Bioorg Chem
November 2021
Drug Design and Synthesis Laboratory, Department of Chemistry, Jamia Millia Islamia, New Delhi 110025, India. Electronic address:
Development of multitargeted ligands have demonstrated remarkable efficiency as potential therapeutics for Alzheimer's disease (AD). Herein, we reported a new series of deoxyvasicinone analogues as dual inhibitor of acetylcholinesterase (AChE) and tau aggregation that function as multitargeted ligands for AD. All the multitargeted ligands 11(a-j) and 15(a-g) were designed, synthesized, and validated by HNMR, CNMR and mass spectrometry.
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!