edoc

1,2-substituted 4-(1H)-quinolones : synthesis, antimalarial and antitrypanosomal activities in vitro

Wube, Abraham and Hüfner, Antje and Seebacher, Werner and Kaiser, Marcel and Brun, Reto and Bauer, Rudolf and Bucar, Franz. (2014) 1,2-substituted 4-(1H)-quinolones : synthesis, antimalarial and antitrypanosomal activities in vitro. Molecules, Vol. 19, H. 9. pp. 14204-14220.

Full text not available from this repository.

Official URL: http://edoc.unibas.ch/dok/A6348381

Downloads: Statistics Overview

Abstract

A diverse array of 4-(1H)-quinolone derivatives bearing substituents at positions 1 and 2 were synthesized and evaluated for antiprotozoal activities against Plasmodium falciparum and Trypanosoma brucei rhodesiense, and cytotoxicity against L-6 cells in vitro. Furthermore, selectivity indices were also determined for both parasites. All compounds tested showed antimalarial activity at low micromolar concentrations, with varied degrees of selectivity against L-6 cells. Compound 5a was found to be the most active against P. falciparum, with an IC50 value of 90 nM and good selectivity for the malarial parasite compared to the L-6 cells. Compound 10a, on the other hand, showed a strong antitrypanosomal effect with an IC50 value of 1.25 µM. In this study side chain diversity was explored by varying the side chain length and substitution pattern on the aliphatic group at position-2 and a structure-antiprotozoal activity study revealed that the aromatic ring introduced at C-2 contributed significantly to the antiprotozoal activities.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Kaiser, Marcel and Brun, Reto
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:MDPI
ISSN:1420-3049
Note:Publication type according to Uni Basel Research Database: Journal article
Related URLs:
Identification Number:
Last Modified:10 Apr 2015 09:12
Deposited On:10 Apr 2015 09:12

Repository Staff Only: item control page