Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
In this study, a 50-membered library of substituted 4-hydroxyquinolin-2(1H)-ones and two closely related analogues was designed, scored in-silico for drug likeness and subsequently synthesized. Thirteen derivatives, all sharing a common 3-phenyl substituent showed minimal inhibitory concentrations against Mycobacterium tuberculosis H37Ra below 10 μM and against Mycobacterium bovis AN5A below 15 μM but were inactive against faster growing mycobacterial species. None of these selected derivatives showed significant acute toxicity against MRC-5 cells or early signs of genotoxicity in the Vitotox™ assay at the active concentration range. The structure activity study relation provided some insight in the further favourable substitution pattern at the 4-hydroxyquinolin-2(1H)-one scaffold and finally 6-fluoro-4-hydroxy-3-phenylquinolin-2(1H)-one (38) was selected as the most promising member of the library with a MIC of 3.2 μM and a CC against MRC-5 of 67.4 μM.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2017.06.061 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Systematic growth of non-epitaxial ZnO shell over Ln-Li co-doped YO phosphor core.
Phys Chem Chem Phys
September 2025
Department of Physics, Indian Institute of Technology (ISM) Dhanbad, Jharkhand-826004, India.
Here, Ln-Li co-doped YO@ZnO core-shell heterostructures were synthesized by three different techniques - intermediate layer conversion method, a hydrothermal method, and an interlayer mediated hydrothermal method. The synthesis procedure is optimized based on the thickness and compactness of the developed shell. The growth kinetics and synthesis mechanism of each adopted method have been explained in detail using XRD, FESEM, TEM, SAED, and EDX characterization techniques.
View Article and Find Full Text PDFHarnessing volatile organic compound biomarkers for early cancer detection: molecular to nanotechnology-based approaches.
Nanoscale
September 2025
School of Biochemical Engineering, Indian Institute of Technology (BHU) Varanasi, Uttar Pradesh 221005, India.
Early-stage cancer diagnosis is considered a grand challenge, and even though advanced analytical assays have been established through molecular biology techniques, there are still clinical limitations. For example, low concentration of target biomarkers at early stages of cancer, background values from the healthy cells, individual variation, and factors like DNA mutations, remain the limiting factor in early cancer detection. Volatile organic compound (VOC) biomarkers in exhaled breath are produced during cancer cell metabolism, and therefore may present a promising way to diagnose cancer at the early stage since they can be detected both rapidly and non-invasively.
View Article and Find Full Text PDFAntiferroelectric SnO Network with Amorphous Surface for Electrochemical N Fixation.
Angew Chem Int Ed Engl
September 2025
State Key Laboratory of Bioinspired Interfacial Materials Science, Bioinspired Science Innovation Center, Hangzhou International Innovation Institute, Beihang University, Hangzhou, 311115, China.
Electrochemical nitrogen fixation-a sustainable pathway for converting abundant N into NH using renewable energy-holds transformative potential for revolutionizing artificial nitrogen cycles. Nevertheless, even the state-of-the-art catalytic systems also suffer from inadequate N adsorption capacity, which critically limits ammonia production rates and Faradaic efficiency (FE). To overcome this bottleneck, we strategically leveraged the antiferroelectric properties of SnO to establish dipole-dipole interactions with N molecules, synergistically enhancing both N adsorption and activation kinetics.
View Article and Find Full Text PDFA water-soluble NIR-II fluorescent probe for non-invasive real-time detection of blood ATP optoacoustic and fluorescence imaging.
J Mater Chem B
September 2025
State Key Laboratory of Luminescent Materials and Devices, Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates, College of Materials Science and Engineering, South China University of Technology, Guangzhou 510640, China.
Adenosine triphosphate (ATP) is a critical biomolecule in cellular energy metabolism, with abnormal levels in the bloodstream linked to pathological conditions such as ischemia, cancer, and inflammatory disorders. Accurate and real-time detection of ATP is essential for early diagnosis and disease monitoring. However, conventional biochemical assays and other techniques suffer from limitations, including invasive sample collection, time-consuming procedures, and the inability to provide dynamic, monitoring.
View Article and Find Full Text PDFMicrofluidic Microspheres Loaded with Aggregation-Induced Emission Nanomicelles for Theranostic Applications in Osteoarthritis.
Adv Healthc Mater
September 2025
State Key Laboratory of Advanced Technology for Materials Synthesis and Processing, Wuhan University of Technology, Wuhan, 430070, P. R. China.
Osteoarthritis (OA) is a common degenerative joint disease, and early diagnosis and effective treatment are essential for managing its progression. This study focuses on the development of a novel drug delivery system using aggregation-induced emission (AIE) probe for enhanced fluorescence imaging and targeted therapy in OA. TPE-S-BTD, an AIE probe, is synthesized and characterized for its photophysical properties, demonstrating significant aggregation-induced fluorescence enhancement.
View Article and Find Full Text PDF