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Design and synthesis of a new class of 4-aminoquinolinyl- and 9-anilinoacridinyl Schiff base hydrazones as potent antimalarial agents

IR@CDRI: CSIR-Central Drug Research Institute, Lucknow

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Field Value
 
Creator Sharma, Moni
Chauhan, Kuldeep
Srivastava, R K
Singh, S V
Srivastava, Kumkum
Saxena, J K
Puri, S K
Chauhan, P M S
 
Date 2014-08-01T11:31:52Z
2014-08-01T11:31:52Z
2014
 
Identifier Chemical Biology & Drug Design, 2014, 84(2), 175-81
http://hdl.handle.net/123456789/1334
 
Description A series of novel 4-aminoquinolinyl and 9-anilinoacridinyl Schiff base hydrazones have been synthesized and evaluated for their antimalarial activity. All compounds were evaluated in vitro for their antimalarial activity against chloroquine-sensitive strain 3D7 and the chloroquine-resistant K1 strain of P. falciparum and for cytotoxicity toward Vero cells. Compounds 17, 20, and 21 displayed good activity against the 3D7 strain with IC50 values ranging from 19.69-25.38 nM. Moreover, compounds 16, 17, 21, 24, 32 and 33 exhibited excellent activities (21.64-54.26 nM) against K1 strain and several compounds displayed β-hematin inhibitory activity, suggesting that, they act on the haem crystallization process like CQ. Compounds were also found to be nontoxic with good selectivity index
 
Format 234842 bytes
application/pdf
 
Language en
 
Relation CSIR-CDRI Communication No. 8600
 
Subject 4-Aminoquinoline
9-Anilinoacridine
Schiff base
Oxalamide
Antimalaria
 
Title Design and synthesis of a new class of 4-aminoquinolinyl- and 9-anilinoacridinyl Schiff base hydrazones as potent antimalarial agents
 
Type Article