Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
View Archive Info| Field | Value | |
| Creator |
Kumar, Ashok
Srivastava, Kumkum Rajakumar, S Puri, S K Chauhan, P M S |
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| Date |
2011-03-17T11:38:10Z
2011-03-17T11:38:10Z 2010 |
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| Identifier |
Bioorg Med Chem Lett 20(23), 7059-7063
http://hdl.handle.net/123456789/651 |
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| Description |
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 standard drug CQ (MIC = 0.125 µg/mL) 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.
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| Format |
110113 bytes
application/pdf |
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| Language |
en
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| Relation |
CDRI Communication no. 7969
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| Subject |
Antimalarial
4-Aminoquinoline quinoline-acridine P. falciparum P. yoelii |
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| Title |
Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents
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| Type |
Article
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