Search results for "4-Quinolones"

Microwave-Assisted Synthesis of Polysubstituted 4-Quinolones from Deprotonated α-Aminonitriles

2010

The α-alkylation of deprotonated N-aryl-α-aminonitriles with α-bromoesters furnishes intermediates that can be cyclized to 4-quinolones upon microwave irradiation. Alternatively, base-induced dehydrocyanation of the alkylation products furnishes enaminoesters, which can, for example, be converted into quinoline-3-carboxylates.

Anti- Toxoplasma Activities of 24 Quinolones and Fluoroquinolones In Vitro: Prediction of Activity by Molecular Topology and Virtual Computational Te…

2000

ABSTRACT The apicoplast, a plastid-like organelle of Toxoplasma gondii , is thought to be a unique drug target for quinolones. In this study, we assessed the in vitro activity of quinolones against T. gondii and developed new quantitative structure-activity relationship models able to predict this activity. The anti- Toxoplasma activities of 24 quinolones were examined by means of linear discriminant analysis (LDA) using topological indices as structural descriptors. In parallel, in vitro 50% inhibitory concentrations (IC 50 s) were determined in tissue culture. A multilinear regression (MLR) analysis was then performed to establish a model capable of classifying quinolones by in vitro acti…

Domino Synthesis of 3-Alkyliden-2,3-Dihydro-4-Quinolones

2019

Cinoxacin complexes with divalent metal ions. Spectroscopic characterization. Crystal structure of a new dinuclear Cd(II) complex having two chelate-…

1998

Several cinoxacin (HCx) complexes with divalent metal ions have been prepared and characterized by spectroscopic techniques. The crystal structure of [Cd 2 (Cx) 4 (H 2 O) 2 ] · 10H 2 O has been determined by X-ray diffraction. The complex is triclinic, space group with unit-cell dimensions: a =10.412(2), b =11.119(2), c =13.143(6)A, α=76.78(4)°, β =74.59(3)°, γ =77.12(3)°, V =1406.0(8) A 3 . In this complex each cadmium atom is heptacoordinated; the metal environment is formed by two O keto and two O carbox atoms from two different cinoxacinate monoanions, two carboxylate oxygen atoms from a third cinoxacinate ligand and by one water oxygen atom on the seventh position. Two of the cinoxacin…

ChemInform Abstract: Microwave-Assisted Synthesis of Polysubstituted 4-Quinolones from Deprotonated α-Aminonitriles.

2011

The α-alkylations of deprotonated Strecker products such as (I) or (V) give a series of intermediates such as (III), (VI), or (X), which undergo microwave-assisted HCN and EtOH eliminations leading to the title quinolones (IV), (VII)/(VIII), or (XI).

GyrA sequence-based typing of Legionella.

2000

Comparative sequence analysis of a 423-bp segment of the gyrA gene including a region homologous to the quinolone resistance-determining region (QRDR) of other species was evaluated as a novel typing method for Legionella strains. The study was performed with 29 reference strains representing 11 different Legionella species, with various serogroups, and with 13 clinical isolates of L. pneumophila. Pulsed-field gel electrophoresis and serotyping were employed for comparison of the clinical isolates. QRDR sequencing proved to be a highly discriminative tool for typing Legionellae, and permitted identification of species, serogroups and even different strains within serogroup 1. None of the is…

Synthesis of 2,3‐Dihydro‐4‐pyridones, 4‐Quinolones, and 2,3‐Dihydro‐4‐azocinones by Visible‐Light Photocatalytic Aerobic Dehydrogenation

2019

Simultaneous identification of campylobacters and prediction of quinolone resistance by comparative sequence analysis.

1997

Comparative sequence analysis of a 30-bp segment in the quinolone resistance-determining region of campylobacters not only allows for the detection of base changes associated with resistance but also is a powerful tool for species identification based on silent mutations.

Prediction of quinolone activity against Mycobacterium avium by molecular topology and virtual computational screening.

2000

ABSTRACT We conducted a quantitative structure-activity relationship study using a database of 158 quinolones previously tested against Mycobacterium avium-M. intracellulare complex in order to develop a model capable of predicting the activity of new quinolones against the M. avium-M. intracellulare complex in vitro. Topological indices were used as structural descriptors and were related to anti- M. avium-M. intracellulare complex activity by using the linear discriminant analysis (LDA) statistical technique. The discriminant equation thus obtained correctly classified 137 of the 158 quinolones, including 37 of a test group of 44 randomly chosen compounds. This model was then applied to 2…