Synthesis and biological screening of some quinolino sulphonamide derivatives

Abstract

The thesis highlights the studies on the synthesis, characterization and biological newlinestudies of quinoline derivatives. newlineThe results were used to find out active compounds and four series of such active newlinecompounds i.e. 4-[3-(substituted phenyl)-5-2-(chloro- quinolin-3-yl)-4,5-dihydro-1Hpyrazole-1-yl] benzene sulfonamide (1a-1j), 4-[3-(substituted phenyl)-5-(2,6-dichloro newlinequinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl] benzene sulfonamide (2k-2t), [5-(2- newlinechloroquinolin-3-yl)-3-(substituted phenyl)-4,5-dihydro-1H-pyrazol-1-yl] -pyridin-3-ylmethanone (3a -3j ) and [5-(2,6-dichloroquinolin-3-yl)-3-(substituted phenyl)-4,5-dihydro1H-pyrazol-1-yl] pyridine-3-yl-methanone (4k -4t ) were synthesized. newlineAll the synthesized compounds were characterized by IR, 1H NMR, 13C NMR, newlineMASS spectrometry and elemental analysis and screened for their invitro antimalarial newlineactivity against Plasmodium falciparum (3D7) and (K1) strain by SYBR Green I- based newlinefluorescence (MSF) assay method. Selectivity index was measured by using IC50 and CC50 newlinevalues of test compounds along with the standard drug i.e. Chloroquine diphosphate. It also newlinedescribes evaluation of the synthesized compounds for their antibacterial and antifungal newlineactivity along with the standard drug i.e. Ciprofloxacin and Fluconazole respectively. newlineResults revealed that among the tested compounds, 1a, 1h, 2k, 2r, 3e , 3j , 4m and newline4o were found to be most active among all the tested compounds. newline