Background: The adverse effects of mefloquine and other quinoline antimalaria drugs can be severe and long-lasting. We believe that the trigger for these effects may be drug-induced hepatocellular damage that causes, firstly, a spillage of retinoids into the circulation (and hence a direct toxic effect on the brain and other target organs), and secondly, disruption of the liver-thyroid axis (an...

The title compound, C20H17F3N2O4, named tasquinimod, is a second-generation oral quinoline-3-carboxamide analogue, which is currently in phase III clinical trials for the treatment of metastatic prostate cancer. The quinoline unit is almost planar (r.m.s. deviation of fitted atoms = 0.0075 Å). The carboxamide side chain, substituted at position 3, is tilted by 88.07 (7)° to the quinoline plane....

Chloroquine is thought to exert its antimalarial effect by preventing the polymerization of toxic heme released during proteolysis of hemoglobin in the Plasmodium digestive vacuole. The mechanism of this blockade has not been established. We incubated cultured parasites with subinhibitory doses of [3H]chloroquine and [3H] quinidine. These [3H]quinoline compounds became associated with hemozoin ...

Nitrogen heterocyclic compounds are used in the pharmaceutical industry, in medicine and in agriculture for their biological activity. 4-Amino-3-acetylquinoline, a new synthetically prepared quinoline derivative, was the most effective compound in our primary cytotoxic screening. In this study, we evaluated cytotoxic/antiproliferative activity of quinoline using murine leukemia cell line L1210....

Identification of the novel (E)-N'-((2-chloro-7-methoxyquinolin-3-yl)methylene)-3-(phenylthio)propanehydrazide scaffold 18 has led to the development of a new series of biologically active hydrazide compounds. The parent compound 18 and new quinoline derivatives 19-26 were prepared from the corresponding quinoline hydrazones and substituted carboxylic acids using EDC-mediated peptide coupling r...

Reports indicating the value of quinidine sulfate in angina pectoris led to (1) a search for related drugs which were equally effective but less toxic, and (2) a study of the mode of action of these drugs. It was found that quinidine, quinine, cinchonadine, and cinchamidine decrease the frequency of attacks in daily life and increase the exercise tolerance as measured by a standardized test. Qu...

In the title compound, C(27)H(18)Cl(2)N(2)O(2), the 2-chloro-quinoline and 6-chloro-quinoline rings are almost planar, with maximum deviations from their mean planes of 0.072 (1) and 0.044 (1) Å, respectively, for the Cl atoms. The inter-planar angle between these rings is 14.36 (5)°. The inter-planar angle between the 6-chloro-quinoline and phenyl rings is 66.00 (8)°. In the crystal, mol-ecule...

Many quinolones, substituted quinolines and thiones are well known for their biological activity. The redox characteristics of such biological substances may provide valuable information about the redox behaviour in living systems. The present paper is aimed at carrying out a methodical cyclic voltammetric investigation of the peak potential values of 4-methyl/phenyl -3vinyl quinoline-2(1H) one...