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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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Field Value
 
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
 
Date 2014-04-21T10:03:49Z
2014-04-21T10:03:49Z
2013
 
Identifier European Journal of Medicinal Chemistry, 2013, 66, 69–81
http://hdl.handle.net/123456789/1206
 
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.
 
Format 415233 bytes
application/pdf
 
Language en
 
Relation CSIR-CDRI Communication No. 8473
 
Subject 4-Aminoquinoline
Chloroquine
Tetrazole
Antimalarial
Cytotoxicity
 
Title Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents
 
Type Article