Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains |
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| Institution: | 1. Department of Studies and Research in Chemistry, University College of Science, Tumkur University, Tumakuru 572103, Karnataka, India;2. Department of Chemistry, Bapatla Engineering College (Autonomous), Acharaya Nagarjuna University Post Graduate Research Centre, Bapatla 522102, Andhra Pradesh, India;3. Department of Chemistry, Bapatla College of Arts and Sciences, Baptla 522101, Andhra Pradesh, India |
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| 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. |
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| Keywords: | 4-Aminoquinoline Antimalarial Heam binding |
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