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| Title: | Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents |
| Authors: | Kumar, Ashok
Srivastava, Kumkum
Kumar, S R
Puri, S K
Chauhan, P M S |
| Keywords: | Antimalarial
4-Aminoquinoline
quinoline-acridine
P. falciparum
P. yoelii. |
| Issue Date: | 2009 |
| Citation: | Bioorg. Med. Chem. Lett, 19 (24), 2009, 6996-6999 |
| Abstract: | Despite 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 P. falciparum. Among the evaluated compounds, compound 17 (MIC = 0.125 µg/mL) was equipotent to CQ and compound 21 (MIC = 0.031 µg/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 P. 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. |
| URI: | http://hdl.handle.net/123456789/578 |
| Appears in Collections: | Medicinal and Process Chemistry
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| chauhanpms-7850-BMCL-2009-19(24)-6996-6999.pdf | | 109Kb | Adobe PDF | View/Open |
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