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Design, Synthesis, Antimalarial Activity and Docking Study of 7-Chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines

Author(s):

Jahnabi Kalita, Dipak Chetia and Mithun Rudrapal*  

Abstract:


Background: Malaria is a growing infectious disease burden due to the increasing emergence of resistant strains of Plasmodium falciparum. Because of limited therapeutic efficacy of available antimalarial drugs, the development of potent antimalarial drug agents is therefore an urgent requirement to fight againt resistant malaria.

Objective: The objective of this work was to develop novel quinoline-baed antimalarial agents that would be active against resistant P. falciparum malaria.

Methods: Some 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines were synthesized for the evaluation of their potential as possible antimalarial agents, particularly against resistant malaria. The antimalarial activity of synthesized compounds was evaluated in vitro against blood stage parasites of P. falciparum. Further, molecular docking and drug-likeness including ADMET (Absorption, Distribution, Metabolism, Elimination and Toxicity) studies were also carried out using in silico tools.

Results: Results reveal the in vitro antimalarial activity of synthesized 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines against P. falciparum. Docking study investigates the antimalarial effectiveness of synthesized quinolines as novel plasmepsin 2 inhibitors. Drug-likeness prediction exhibits acceptable drug-likeness and ADMET properties.

Conclusion: Based upon our findings, it is concluded that the molecular scaffold of 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines may be used as a lead structure for further modification in search of more still potent antimalarial drug molecules.

Keywords:

Malaria, P. falciparum, Drug resistance, 7-Chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines, Antimalarial, Plasmepsin 2 inhibitors

Affiliation:

Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh - 786 004, Assam, Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh - 786 004, Assam, Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh - 786 004, Assam



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