Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 129, Issue -, Pages 175-185Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.02.024
Keywords
Aminoquinoline; Antimalarial activity; Heme binding activity; Docking studies
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Funding
- SERB, Govt. of India, New Delhi [EMR/2014/001127]
- CSIR
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A series of novel N-substituted 4-aminoquinoline-pyrimidine hybrids have been synthesized via simple and economic route and evaluated for their antimalarial activity. Most compounds showed potent antimalarial activity against both CQ-sensitive and CQ-resistant strains with high selectivity index. All the compounds were found to be non-toxic to the mammalian cell lines. The most active compound 7b was analysed for heme binding activity using UV-spectrophotometer. Compound was found to interact with heme and a complex formation between compound and heme in a 1:1 stoichiometry ratio was determined using job plots. The interaction of these hybrids was also investigated by the molecular docking studies in the binding site of wild type Pf-DHFR-TS and quadruple mutant Pf-DHFR-TS. The pharmacokinetic property analysis of best active compounds was also studied by ADMET prediction. (C) 2017 Elsevier Masson SAS. All rights reserved.
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