nystatin-a1 and quinoline

Mitochondria play central roles in plenty of biological processes, such as apoptosis, signaling, and cell differentiation. Mitochondrial depolarization is a significant sign of deterioration of intracellular status. Although many fluorescent probes for visualizing mitochondria have been delivered, two-photon red-emitting mitochondrial probes capable of detecting mitochondrial depolarization remain rare. In this work, by linking a pyrene moiety to a quinoline salt, we have constructed two-photon red-emitting mitochondrial probes, MVQ and HVQ. Between them, HVQ with a longer side chain exhibits higher hydrophobic properties, and can image mitochondria with high-fidelity due to the aggregation caused quenching effect. In cooperation with MTDR, a commercialized mitochondrial probe, HVQ, could be used to image the depolarization of mitochondria induced by a protonophore and hydrogen peroxide. We believe that HVQ can serve as a powerful tool for the investigation of mitochondria and mitochondrial membrane potential in fundamental biological research.

Topics: Fluorescence Resonance Energy Transfer; Fluorescent Dyes; Hep G2 Cells; Humans; Hydrogen Peroxide; Membrane Potential, Mitochondrial; Mitochondria; Models, Molecular; Molecular Conformation; Nystatin; Photons; Pyrenes; Quinolines

An improved domino/Knoevenagel-hetero-Diels-Alder reaction of two new aldehyde substrates; 7-olefinoxy-coumarin-8-carbaldehyde and 2-alkensulfanyl-quinoline-3-carbaldehyde, with pyrazolones was studied in ionic liquid triethylammonium acetate (TEAA), affording a series of pyrazolopyran annulated-pyrano-fused coumarins, and thiopyrano-fused quinolones. Besides acting as catalyst, since no additional catalyst used, the ionic liquid TEAA also promised its easy recovery. In all new polyheterocycles, the cis-fusion of two pyranyl rings had been inferred from 2D NMR COSY and NOESY experiments. All are good antitubercular agents, as they are found active against Mycobacterium tuberculosis H37Rv, and antibacterial agents, as they are found active against three Gram-positive (Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis) and three Gram-negative (Salmonella typhi, Vibrio cholerae, Escherichia coli) bacteria.

Topics: Aldehydes; Anti-Bacterial Agents; Coumarins; Gram-Negative Bacteria; Gram-Positive Bacteria; Heterocyclic Compounds; Ionic Liquids; Microbial Sensitivity Tests; Mycobacterium tuberculosis; Pyrans; Pyrazolones; Quinolines; Structure-Activity Relationship

A highly improved one-pot procedure for the synthesis of diazepinones, which incorporate a bioactive quinoline nucleus, under catalyst-, and solvent-free environment has been developed. The method allowed us to achieve the products in high yields without requiring a chromatographic separation. All new quinolyldibenzo[b,e][1,4]diazepinones 6a-h thus obtained were further treated to achieve N10-allylated products 7a-h by a simple allylation. The structure of all new synthesized compounds was established based on elemental analysis, mass, (1)H NMR, (13)C NMR, IR spectral data, 2D NMR experiments, and single crystal X-ray study. From in vitro antimicrobial activity studies it revealed all are active against Gram positive (Streptococcus pneumoniae, Clostridium tetani, and Bacillus subtilis), Gram negative (Salmonella typhi, Vibrio chlolerae and Escherichia coli), M. Tuberculosis H37RV bacteria, and fungus like Candia albicans and Aspergillus fumigatus. All were also found to display good antioxidant activity of a ferric reducing power.

Topics: Anti-Infective Agents; Antioxidants; Azepines; Crystallography, X-Ray; Fungi; Gram-Negative Bacteria; Gram-Positive Bacteria; Microbial Sensitivity Tests; Molecular Conformation; Quinolines