Optimization of endochin-like quinolones for antimalarial activity
نویسندگان
چکیده
منابع مشابه
Endochin-like quinolones are highly efficacious against acute and latent experimental toxoplasmosis.
Toxoplasma gondii is a widely distributed protozoan pathogen that causes devastating ocular and central nervous system disease. We show that the endochin-like quinolone (ELQ) class of compounds contains extremely potent inhibitors of T. gondii growth in vitro and is effective against acute and latent toxoplasmosis in mice. We screened 50 ELQs against T. gondii and selected two lead compounds, E...
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The historical antimalarial compound endochin served as a structural lead for optimization. Endochin-like quinolones (ELQ) were prepared by a novel chemical route and assessed for in vitro activity against multidrug resistant strains of Plasmodium falciparum and against malaria infections in mice. Here we describe the pathway to discovery of a potent class of orally active antimalarial 4(1H)-qu...
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The formation of hemozoin (malaria pigment) has been proposed as an ideal drug target for antimalarial screening programs. In this study, we used an improved, cost-effective and high-throughput spectrophotometric assay to screen plant extracts for finding novel antimalarial plant sources. Fifteen extracts with different polarity from three Iranian Artemisia species, A. ciniformis, A. biennis an...
متن کاملScreening of Different Extracts from Artemisia Species for Their Potential Antimalarial Activity
The formation of hemozoin (malaria pigment) has been proposed as an ideal drug target for antimalarial screening programs. In this study, we used an improved, cost-effective and high-throughput spectrophotometric assay to screen plant extracts for finding novel antimalarial plant sources. Fifteen extracts with different polarity from three Iranian Artemisia species, A. ciniformis, A. biennis an...
متن کاملAnti-Mycobacterium avium activity of quinolones: structure-activity relationship studies.
The structures and inhibitory activities of 88 quinolones, previously studied as potential in vitro inhibitors of 14 selected strains of Mycobacterium avium complex, were examined in an effort to identify a quinolone with optimal activity towards all strains. A MULTICASE structure-activity relationship analysis of the inhibitory activities of these 88 quinolones against 14 strains of M. avium w...
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ژورنال
عنوان ژورنال: Experimental Parasitology
سال: 2011
ISSN: 0014-4894
DOI: 10.1016/j.exppara.2010.10.016