Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents

Patel, Kuldeep, Karthikeyan, Chandrabose, Hari Narayana Moorthy, N. S., Deora, Girdhar Singh, Solomon, Viswas Raja, Lee, Hoyun and Trivedi, Piyush (2012) Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents. Medicinal Chemistry Research, 21 8: 1780-1784. doi:10.1007/s00044-011-9694-1


Author Patel, Kuldeep
Karthikeyan, Chandrabose
Hari Narayana Moorthy, N. S.
Deora, Girdhar Singh
Solomon, Viswas Raja
Lee, Hoyun
Trivedi, Piyush
Title Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents
Journal name Medicinal Chemistry Research   Check publisher's open access policy
ISSN 1054-2523
1554-8120
Publication date 2012-08
Sub-type Article (original research)
DOI 10.1007/s00044-011-9694-1
Open Access Status
Volume 21
Issue 8
Start page 1780
End page 1784
Total pages 5
Place of publication Basel, Switzerland
Publisher Birkhaeuser Science
Language eng
Formatted abstract
A novel series of 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones were designed, synthesized and screened for antiplasmodial activity. Eleven compounds of the series exhibited micromolar potency against chloroquine sensitive and chloroquine resistant strains. The most potent compound 4-hydroxy-3-(3-(4-nitrophenyl)acryloyl)-2H-chromen-2-one showed inhibitory potency (IC50) of 3.1 and 4 μg/ml against chloroquine sensitive and chloroquine resistant strains, respectively. A structure activity relationship study was performed by correlating the effect of substituents with the antimalarial activity of the title compounds. The novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones reported here should be good lead for further development of antimalarial agents that can overcome resistance.
Keyword Antimalarial
Chalcones
Coumarin
Chalcone derivatives
Antiplasmodial activity
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Pharmacy Publications
 
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