Theses (MSc. Molecular Medicine)

A series of six quinoline derivatives (S1-S6) were synthesized and characterised using FT-IR, 1H-NMR, 13C-NMR studies. Further, the exact molecular mass of the compounds was identified based on the HRMS data using ESI mode of analysis. The synthesized compounds underwent biological evaluation by assessing their in vitro antimalarial activity against malarial strains PF3D7 and PF5202. It was determined by relative fluorescent unit of infected red blood cells treated with 100μM of each synthesized compound. Artesunate was used as a control. Significant antimalarial activity was observed with five of the six compounds synthesized (S1, S2, S3, S4, S6) comparable to that of artesunate. The observed antimalarial activity was probably due to the presence of bioactive antimalarial pharmacophores, such as sulfonyl and quinolinyl moieties respectively. The relative comparison of the structural features of the compounds, compounds with fluorine atom substitutions less than or equal to three exhibited potential activity, than the compound 5 with six fluorine atoms substituted as di-substituted trifluoromethyl groups. Due to excess hydrophobicity, the cell permeation might be affected that led to the relatively inactive nature of the compound. Keywords: quinoline derivatives, in vitro antimalarial activity