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Published on: July 11, 2025
Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains
Srinivasarao Kondaparla1, Awakash Soni2, Ashan Manhas2
1Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
Abstract:
In the present study we have synthesized a new class of 4-aminoquinolines and evaluated against Plasmodium falciparum in vitro (3D7-sensitive strain & K1-resistant strain) and Plasmodium yoelii in vivo (N-67 strain). Among the series, eleven compounds (5, 6, 7, 8, 9, 11, 12, 13, 14, 15 and 21) showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogues showed 100% suppression of parasitemia on day 4 in the in vivo mouse model against N-67 strain when administered orally. Further, biophysical studies suggest that this series of compounds act on heme polymerization target.

