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. 2017 Feb:70:74-85.
doi: 10.1016/j.bioorg.2016.11.010. Epub 2016 Nov 23.

Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains

Srinivasarao Kondaparla  1 , Awakash Soni  2 , Ashan Manhas  2 , Kumkum Srivastava  2 , Sunil K Puri  2 , S B Katti  3
Affiliations

Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains

Srinivasarao Kondaparla et al. Bioorg Chem. 2017 Feb.

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.

Keywords: 4-Aminoquinoline; Antimalarial; Heam binding; Plasmodium falciparum.

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