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Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains.
- Source :
-
Bioorganic Chemistry . Feb2017, Vol. 70, p74-85. 12p. - Publication Year :
- 2017
-
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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00452068
- Volume :
- 70
- Database :
- Academic Search Index
- Journal :
- Bioorganic Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 122119654
- Full Text :
- https://doi.org/10.1016/j.bioorg.2016.11.010