Synthesis and Antimalarial Activity of Triazole Hybrids: Recent Developments and Structure–Activity Relationships

ABSTRACT The rise of drug or multidrug resistance in Plasmodia strains has made malaria the most important tropical parasitic disease. To address this issue, new antimalarial drugs must be developed. As a fundamental building block in organic synthesis, materials science, and pharmaceutical chemistry, the triazole scaffold is an essential part of heterocyclic chemistry. Because of their broad chemical properties and potential biological applications, including antimalarial, the synthesis of triazoles has gained significant attention in the field of organic chemistry. This review primarily focuses on the synthesis, the wide range of antimalarial activities of several hybridized 1,2,3‐triazoles and 1,2,4‐triazoles, and the structure–activity relationships (SAR) reported since 2022, which target various stages of the Plasmodium life cycle. Because of their adaptability, they are extremely efficient against both drug‐sensitive and drug‐resistant strains of P. falciparum , making them indispensable resources in areas where resistance is common. Even higher antimalarial effectiveness has been achieved by the synergistic effects of mixing the triazole moiety with additional pharmacophores. This strategy may be able to surpass current resistance mechanisms and offer a more long‐lasting way to treat malaria. Triazole hybrid compounds continue to play a significant role in malarial chemotherapy despite the development of numerous antimalarial leads. Researchers can further investigate and innovate in the synthesis, antimalarial evaluation, and structure–activity relationship (SAR) studies of triazoles as pharmaceuticals by including them as crucial components in drug discovery, thereby examining their potential therapeutic importance.