4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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Creator |
Kumar, Ashok
Srivastava, Kumkum Rajakumar, S Siddiqi, M I Puri, S K Sexana, J K Chauhan, P M S |
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Date |
2011-03-18T08:22:40Z
2011-03-18T08:22:40Z 2010 |
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Identifier |
European Journal of Medicinal Chemistry 46(2), 11, 676-690
http://hdl.handle.net/123456789/652 |
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Description |
A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity towards VERO cell line. Five compounds (19, 20, 23, 41 and 45) exhibited the antimalarial potency superior to CQ. Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg x 4 days against CQ-resistant strain of P. Yoelii. Inhibition of β-hematin formation assay and molecular docking study has been conducted in order to gain insight into the mechanism of action of proposed targets for the 4-anilinoquinoline and triazine moiety of the hybrid compounds
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562046 bytes
application/pdf |
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Language |
en
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Relation |
CDRI Communication No 7995
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Subject |
4-Anilinoquinoline triazine
Antimalarial P. Falciparum P. Yoelii |
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Title |
4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents
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Type |
Article
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