Publication: SYNTHESIS, CHARACTERISATION AND BIOLOGICAL EVALUATION OF A SERIES OF NOVEL QUINOLINE DERIVATIVES AS POTENTIAL ANTIMALARIAL AGENTS
Date
2022
Authors
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Publisher
International Medical University
Abstract
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
Description
Keywords
In Vitro Techniques, Antimalarials, Fluorine, Malaria, Plasmodium