biostudies-literatureUnknown15(2)Barmade MAUniversity Grants CommissionDepartment of Biotechnology, Ministry of Science and Technology, IndiaThe emergence of drug resistance against the frontline antimalarials is a major challenge in the treatment of malaria. In view of emerging reports on drug-resistant strains of <i>Plasmodium</i> against artemisinin combination therapy, a dire need is felt for the discovery of novel compounds acting against novel targets in the parasite. In this study, we identified a novel series of quinolinepiperazinyl-aryltetrazoles (QPTs) targeting the blood stage of <i>Plasmodium</i>. <i>In vitro</i> anti-plasmodial activity screening revealed that most of the compounds showed IC₅₀ < 10 μM against chloroquine-resistant <i>Pf</i>INDO strain, with the most promising lead compounds 66 and 75 showing IC₅₀ values of 2.25 and 1.79 μM, respectively. Further, compounds 64-66, 68, 75-77 andRSC medicinal chemistry572-594https://www.ebi.ac.uk/biostudies/studies/S-EPMC10880932biostudies-literatureNovel quinolinepiperazinyl-aryltetrazoles targeting the blood stage of <i>Plasmodium falciparum</i>.PMC10880932Yadav MRRana BSahal DBarmade MAAgrawal PRajput SRMurumkar PRfalseNovel quinolinepiperazinyl-aryltetrazoles targeting the blood stage of <i>Plasmodium falciparum</i>.The emergence of drug resistance against the frontline antimalarials is a major challenge in the treatment of malaria. In view of emerging reports on drug-resistant strains of <i>Plasmodium</i> against artemisinin combination therapy, a dire need is felt for the discovery of novel compounds acting against novel targets in the parasite. In this study, we identified a novel series of quinolinepiperazinyl-aryltetrazoles (QPTs) targeting the blood stage of <i>Plasmodium</i>. <i>In vitro</i> anti-plasmodial activity screening revealed that most of the compounds showed IC₅₀ < 10 μM against chloroquine-resistant <i>Pf</i>INDO strain, with the most promising lead compounds 66 and 75 showing IC₅₀ values of 2.25 and 1.79 μM, respectively. Further, compounds 64-66, 68, 75-77 and2024-01-01T00:00:00Z2024 Feb2026-06-03T00:24:31.145Z2025-04-04T23:31:40.049ZS-EPMC108809323838988810.1039/d3md00417a