The development of drug resistance in malaria parasites is one of the most critical problems with malaria control.

Heterocycles play an essential role in designing and discovering novel malaria-active compounds.

Various N-containing heterocycles such as pyrazole and pyrazoline derivatives have been broadly studied for antimalarial potency in recent years.

Summary of the recent developments in antimalarial activities of pyrazole and pyrazoline derivatives bearing quinoline, pyran, pyrazoline, pyridine, pyrimidine, imidazopyridazine, diazepine, curcumin, thiazole, benzothiazole, thiazolidine, triazine, oxadiazole, chalcone, furan, and the aryl moiety were discussed.

Malaria poses a severe public health risk and a significant economic burden in disease-endemic countries. One of the most severe issues in malaria control is the development of drug resistance in malaria parasites. The standard treatment for malaria is artemisinin-combination therapy (ACT). Nevertheless, the Plasmodium parasite's extensive resistance to prior drugs and reduced ACT efficiency necessitates novel drug discovery. The progress in discovering novel, affordable, and effective antimalarial agents is significant in combating drug resistance, and the hybrid drug concept can be used to covalently link two or more active pharmacophores that may act on multiple targets. Pyrazole and pyrazoline derivatives are considered pharmacologically necessary active heterocyclic scaffolds that possess almost all types of pharmacological activities. This review summarized recent progress in antimalarial activities of synthesized pyrazole and pyrazoline derivatives. The studies published since 2000 are included in this systematic review. This review is anticipated to be beneficial for future study and new ideas in searching for rational development strategies for more effective pyrazole and pyrazoline derivatives as antimalarial drugs.

Pyrazoles

Pyrazolines

Malaria

Antimalarial potency

Parasite

Plasmodium falciparum

No data was used for the research described in the article.

© 2022 The Authors. Published by Elsevier B.V.