| Literature DB >> 27908538 |
Srinivasarao Kondaparla1, Awakash Soni2, Ashan Manhas2, Kumkum Srivastava2, Sunil K Puri2, S B Katti3.
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.Entities:
Keywords: 4-Aminoquinoline; Antimalarial; Heam binding; Plasmodium falciparum
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Year: 2016 PMID： 27908538 DOI： 10.1016/j.bioorg.2016.11.010
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275