Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 3, Pages 607-610Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.12.014
Keywords
N-Hydroxyquinolinone; Anti-plasmodial activity; Anti-bacterial activity; Iron chelation
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Funding
- Ministry of Education (MOE)
- National University of Singapore
- Agency for Science Technology and Research (A/STAR) [JCO-10/03/FG/06/02]
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A 26-member library of novel N-hydroxyquinolinone derivatives was synthesized by a one-pot Buchwald-type palladium catalyzed amidation and condensation sequence. The design of these rare scaffolds was inspired from N-hydroxypyridones and 2-quinolinones classes of compounds which have been shown to have rich biological activities. The synthesized compounds were evaluated for their anti-plasmodial and anti-bacterial properties. In addition, these compounds were screened for their iron(II)-chelation properties. Notably, four of these compounds exhibited anti-plasmodial activities comparable to that of the natural product cordypyridone B. (C) 2014 Elsevier Ltd. All rights reserved.
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