Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents

Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents

Molecular hybridization is a drug discovery strategy that involves the rational design of new chemical entities by the fusion (usually via a covalent linker) of two or more drugs, both active compounds and/or pharmacophoric units recognized and derived from known bioactive molecules. The expected ou...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Vol. 26; no. 13; p. 4093
Main Authors: Vinindwa, Bonani, Dziwornu, Godwin Akpeko, Masamba, Wayiza
Format: Journal Article
Language:English
Published: Basel MDPI AG 05-07-2021
MDPI
Subjects:
Antibiotics
Antiprotozoal agents
chalcones
Chemical modification
Chloroquine
Design
Drug development
Drugs
Enzymes
Hybridization
Hybrids
Malaria
molecular hybrids
Natural products
P. falciparum
Parasites
Quinoline
quinoline-sulfonamide
Selectivity
Side effects
East Asia
Africa
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Summary:Molecular hybridization is a drug discovery strategy that involves the rational design of new chemical entities by the fusion (usually via a covalent linker) of two or more drugs, both active compounds and/or pharmacophoric units recognized and derived from known bioactive molecules. The expected outcome of this chemical modification is to produce a new hybrid compound with improved affinity and efficacy compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profiles, different and/or dual modes of action, reduced undesired side effects and ultimately lead to new therapies. In this study, molecular hybridization was used to generate new molecular hybrids which were tested against the chloroquine sensitive (NF54) strain of P. falciparum. To prepare the new molecular hybrids, the quinoline nucleus, one of the privileged scaffolds, was coupled with various chalcone derivatives via an appropriate linker to produce a total of twenty-two molecular hybrids in 11%–96% yield. The synthesized compounds displayed good antiplasmodial activity with IC50 values ranging at 0.10–4.45 μM.
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ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26134093