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Evaluation of antiplasmodial potential of C-2 and C-8 modified quinolines: in vitro and in silico study.

Medicinal Chemistry 2018 October 16
BACKGROUND: Malaria remains a common life-threatening infectious disease across the globe due to the development of resistance by Plasmodium parasite against most antimalarial drugs. The situation demands new and effective drug candidates against Plasmodium.

OBJECTIVES: The objective of this study is to design, synthesize and test novel quinoline based molecules against the malaria parasite.

METHOD: C-2 and C-8 modified quinoline analogs obtained via C-H bond functionalization approach were synthesized and evaluated for inhibition of growth of P. falciparum grown in human red blood cells using SYBR Green microtiter plate based screening. Computational molecular docking studies were carried out with top fourteen molecules using Autodoc software.

RESULT: The biological evaluation results revealed good activity of quinoline-8-acrylate 3f (IC50 14.2 µM), 2-quinoline-α-hydroxypropionates 4b (IC50 6.5 µM), 4j (IC50 5.5 µM) and 4g (IC50 9.5 µM), and against chloroquine sensitive pf 3D7 strain. Top fourteen molecules were screened also against chloroquine resistant Pf INDO strain and the observed resistant indices were found to lie between 1 and 7.58. Computational molecular docking studies indicated a unique mode of binding of these quinolines to Falcipain 2 and heme moiety, indicating these to be probable targets of their antiplasmodial action.

CONCLUSION: An important finding of our work is the fact that unlike chloroquine which shows a resistance Index of 15, the resistance indices for the most promising molecules studied by us were about one indicating equal potency against drug sensitive and resistant strains of malaria parasite.

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