Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 86, Issue -, Pages 113-121Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.08.053
Keywords
Click chemistry; Ferrcenylchalcone-beta-lactam conjugates; 1H-1,2,3-triazoles; Structure-activity relationship; Plasmodium falciparum
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Funding
- Department of Science and Technology, New Delhi under Innovation in Science Pursuit for Inspired Research (INSPIRE) Fellowship [IF-10482]
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A series of ferrocenylchalcone-beta-lactam conjugates were synthesized and evaluated against 3D7 (CQ-Sensitive) and W2 (CQ-Resistant) strains of Plasmodium falciparum. The SAR studies revealed the dependence of activities at N-1 substituent of beta-lactam ring with compounds being more potent on resistant strain. The compound 9f and 9l with N-cyclohexyl substituent proved to be the most potent and non-cytotoxic among the series exhibiting IC50 values of 2.36 and 2.43 mu M respectively, against W2 strain of P. falciparum. (C) 2014 Elsevier Masson SAS. All rights reserved.
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