Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 2, Pages 745-751Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.11.022
Keywords
Acdridne containing chalcones; Plasmodium falciparum NF-54; Plasmodium yoelii N-67
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Funding
- Ministry of Human Resource Development (MHRD), New Delhi
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A series of novel chalcones bearing acridine moiety attached to the amino group in their ring A have been synthesized through noncatalyzed nucleophilic aromatic substitution reaction between various 3'-aminochalcone or 4'-aminochalcones and 9-chloroacridine. The synthesized chalcone derivatives have been characterized and screened for in vitro antimalarial activity against Plasmodium falciparum NF-54. All the chalcones showed complete inhibition at concentration of 10 mu g/mL and above while three compounds showed significant inhibition at concentration of 2 mu g/mL The three most active chalcone derivatives were screened for in vivo activity as well, but no significant inhibition in parasitaemia was observed when given intraperitoneally to Plasmodium yoelii infected mice model. (C) 2009 Elsevier Masson SAS. All rights reserved.
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