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Issue 1, 2012
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Synthesis of hybrid 4-anilinoquinoline triazines as potent antimalarial agents, their in silico modeling and bioevaluation as Plasmodium falciparumtransketolase and β-hematin inhibitors

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Abstract

Analogues of a novel class of hybrid 4-anilinoquinoline triazines have been synthesized with the aim of identifying the compounds with improved antimalarial activity preserving the potency of parent drug chloroquine (CQ). All the synthesized molecules were evaluated in vitro for their antimalarial activity against chloroquine-sensitive 3D7 and chloroquine-resistant K1 strains of P. falciparum. Molecules were also screened for their cytotoxicity towards VERO cell line. Sixteen compounds (17, 19, 26, 27, 29, 31, 32, 33, 35, 36, 37, 39, 40, 49, 50, and 52) exhibited excellent antimalarial activity with IC50 values ranging from 1.36–4.63 ng ml−1 and were also found to be nontoxic with good selectivity index. In silico activity prediction as well as enzyme inhibitory activity against P. falciparumtransketolase reveals that the molecules are also good inhibitors of the enzymeP. falciparumtransketolase. The compound 52 showed good in vivo activity by oral route and resulted in survival of 3 out of 5 mice till day 28.

Graphical abstract: Synthesis of hybrid 4-anilinoquinoline triazines as potent antimalarial agents, their in silico modeling and bioevaluation as Plasmodium falciparumtransketolase and β-hematin inhibitors

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Publication details

The article was received on 22 Jul 2011, accepted on 17 Sep 2011 and first published on 03 Nov 2011


Article type: Concise Article
DOI: 10.1039/C1MD00188D
Med. Chem. Commun., 2012,3, 71-79

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    Synthesis of hybrid 4-anilinoquinoline triazines as potent antimalarial agents, their in silico modeling and bioevaluation as Plasmodium falciparumtransketolase and β-hematin inhibitors

    M. Sharma, K. Chauhan, S. S. Chauhan, A. Kumar, S. V. Singh, J. K. Saxena, P. Agarwal, K. Srivastava, S. Raja Kumar, S. K. Puri, P. Shah, M. I. Siddiqi and P. M. S. Chauhan, Med. Chem. Commun., 2012, 3, 71
    DOI: 10.1039/C1MD00188D

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