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4-Aminoquinoline hybrids' synthesis and antimalarial activity: A key review.

Created on 06 Aug 2026

Authors

Lekkala Ravindar, Lekkala Revathi, Narmeta Bhasker, Yee Ling Lau

Published in

European journal of medicinal chemistry. Volume 318. Pages 119196. Aug 03, 2026. Epub Aug 03, 2026.

Abstract

One of the deadliest illnesses to spread around the world is malaria, which is caused by different strains of Plasmodium. Effective antimalarial drugs have been developed using a variety of N-heterocyclic moieties. Among these, the 4-aminoquinoline scaffold is crucial for antimalarial activity, not merely because it has been widely used. 4-Aminoquinoline's low toxicity, high tolerance, and quick absorption upon addition have made it a significant antimalarial drug since the 1960s. For traditional antimalarial drugs like chloroquine, the 4-aminoquinoline moiety serves as the fundamental pharmacological scaffold. Its primary significance comes from its ability to precisely localize inside the parasite's digestive vacuole and prevent free heme from being detoxified. Over the years, a number of researchers have been hired to analyse molecular hybridization techniques for the development of combination medications to combat the parasite's resistance to the current drugs. Hence, the current review summarizes some of the major contributions made to the synthesis and antimalarial activity of 4-aminoquinoline hybrids since 2022. A comprehensive analysis of current compounds may also provide new ideas for the construction of anti-malarial drugs that are more effective than those that have already been developed.

PMID:
42556025
Bibliographic data and abstract were imported from PubMed on 06 Aug 2026.

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