Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
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Creator |
Pandey, Shashi
Agarwal, Pooja Srivastava, Kumkum Kumar, Raja Puri, S K Verma, Pravesh Saxena, J K Sharma, Abhisheak Lal, Jawahar Chauhan, P M S |
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Date |
2014-04-21T10:03:49Z
2014-04-21T10:03:49Z 2013 |
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Identifier |
European Journal of Medicinal Chemistry, 2013, 66, 69–81
http://hdl.handle.net/123456789/1206 |
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Description |
A series of novel tetrazole derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activities against both chloroquine-senstive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum as well as for cytotoxicity against VERO cell lines. Most of the synthesized compounds exhibited potent antimalarial activity as compared to chloroquine against K1-strain. Compounds with significant in vitro antimalarial activity were then evaluated for their in vivo efficacy in Swiss mice against P. yoelii following both intraperitoneal (ip) and oral administration, wherein compounds 20 and 23 each showed in vivo suppression of 99.99% parasitaemia on day 4.
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415233 bytes
application/pdf |
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Language |
en
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Relation |
CSIR-CDRI Communication No. 8473
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Subject |
4-Aminoquinoline
Chloroquine Tetrazole Antimalarial Cytotoxicity |
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Title |
Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents
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Type |
Article
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