| Literature DB >> 27688182 |
Amandeep Singh1, Jiri Gut2, Philip J Rosenthal2, Vipan Kumar3.
Abstract
A series of aliphatic and aromatic substituted 1H-1,2,3-triazole-tethered 4-amino-quinoline-ferrocenylchalcone conjugates has been synthesized and evaluated for anti-plasmodial activity. The conjugates with flexible aliphatic (aminoethanol or aminopropanol) substituents on the quinoline ring showed better anti-plasmodial activities compared to those with cyclic (piperazine or aminophenol) substituents. The conjugate 17j was the most potent and non-cytotoxic, with an IC50 value of 0.37 μM against the chloroquine-resistant W2 strain of Plasmodium falciparum. Copyright ÂEntities:
Keywords: 1,3-dipolar cycloaddition; 4-Amino-quinoline-ferrocenylchalcone; Antiplasmodial activities; Structure-activity relationship
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Year: 2016 PMID: 27688182 DOI: 10.1016/j.ejmech.2016.09.044
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514