Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 13, Pages 3618-3628Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.04.010
Keywords
Cadiolides; Antibacterial; Butenolides; Multicomponent; Natural products
Funding
- Region Haute Normandie
- Spanish Ministry of Economy and Competiveness [SAF2011-23777]
- European Regional Development Fund (FEDER)
- Generalitat Valenciana [GVACOMP2014-006, PROMETEO II/2013/014]
- Spanish Ministry of Education, Culture and Sport from FPU program
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The one-pot multicomponent synthesis of natural butenolides named cadiolides A, B, C and analogues has been realized. The antibacterial structure activity relationship shows that the presence of phenolic hydroxyl groups and the number and position of bromine atoms on the different aromatic rings are important features for antibacterial activity, besides it was demonstrated the tolerance of both benzene and furan ring at position 3 of the butenolide nucleus. Furthermore, none of the most relevant antibacterial compounds showed any cytotoxicity in freshly isolated human neutrophils. (C) 2015 Elsevier Ltd. All rights reserved.
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