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pubmed-article:20951034pubmed:abstractTextDespite emergence of resistance to CQ and other 4-aminoquinoline drugs in most of the endemic regions, research findings provide considerable support that there is still significant potential to discover new affordable, safe, and efficacious 4-aminoquinoline antimalarials. In present study, new side chain modified 4-aminoquinoline derivatives and quinoline-acridine hybrids were synthesized and evaluated in vitro against NF 54 strain of Plasmodium falciparum. Among the evaluated compounds, compound 17 (MIC=0.125 ?g/mL) was equipotent to standard drug CQ (MIC=0.125 ?g/mL) and compound 21 (MIC=0.031 ?g/mL) was four times more potent than CQ. Compound 17 showed the curative response to all the treated swiss mice infected with CQ-resistant N-67 strain of Plasmodium yoelii at the doses 50 mg/kg and 25 mg/kg for four days by intraperitoneal route and was found to be orally active at the dose of 100 mg/kg for four days. The promising antimalarial potency of compound 17 highlights the significance of exploring the privileged 4-aminoquinoline class for new antimalarials.lld:pubmed
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pubmed-article:20951034pubmed:authorpubmed-author:RybaDDlld:pubmed
pubmed-article:20951034pubmed:authorpubmed-author:KumarAshokAlld:pubmed
pubmed-article:20951034pubmed:authorpubmed-author:ChauhanPrem...lld:pubmed
pubmed-article:20951034pubmed:authorpubmed-author:SrivastavaKum...lld:pubmed
pubmed-article:20951034pubmed:authorpubmed-author:KumarS RajaSRlld:pubmed
pubmed-article:20951034pubmed:copyrightInfoCopyright © 2010. Published by Elsevier Ltd.lld:pubmed
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pubmed-article:20951034pubmed:year2010lld:pubmed
pubmed-article:20951034pubmed:articleTitleSynthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents.lld:pubmed
pubmed-article:20951034pubmed:affiliationDivision of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow, India.lld:pubmed
pubmed-article:20951034pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:20951034pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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