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Evaluation of Antiplasmodial Potential of C-2 and C-8 Modified Quinolines: in vitro and in silico Study

Author(s):

Rakesh Kumar, Ritika Sharma, Inder Kumar, Pooja Upadhyay, Ankit Kumar Dhiman, Rohit Kumar, Rakesh Kumar, Rituraj Purohit*, Dinkar Sahal* and Upendra Sharma*   Pages 1 - 11 ( 11 )

Abstract:


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

Keywords:

Quinolines, antiplasmodial activity, Plasmodium falciparum, resistance index, docking study.

Affiliation:

Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061, Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061, Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061, Malaria Drug Discovery Laboratory, International Centre for Genetic Engineering and Biotechnology, Aruna Asaf Ali Marg, New Delhi, 110067, Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061, Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061, Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061, Academy of Scientific and Innovative Research, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh-176 061, Malaria Drug Discovery Laboratory, International Centre for Genetic Engineering and Biotechnology, Aruna Asaf Ali Marg, New Delhi, 110067, Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061



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