An amidation/cyclization approach to the synthesis of N-hydroxyquinolinones and their biological evaluation as potential anti-plasmodial, anti-bacterial, and iron(II)-chelating agents
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An amidation/cyclization approach to the synthesis of N-hydroxyquinolinones and their biological evaluation as potential anti-plasmodial, anti-bacterial, and iron(II)-chelating agents
An amidation/cyclization approach to the synthesis of N-hydroxyquinolinones and their biological evaluation as potential anti-plasmodial, anti-bacterial, and iron(II)-chelating agents
Teng, Y. B.; Suwanarusk, R.; Ngai, M. H.; Srinivasan, R.; Ong, A. S. M.; Ho, B.; Rénia, L.; Chai, C. L. L., An amidation/cyclization approach to the synthesis of N-hydroxyquinolinones and their biological evaluation as potential anti-plasmodial, anti-bacterial, and iron(II)-chelating agents. Bioorganic & Medicinal Chemistry Letters 2015, 25 (3), 607-610.
Abstract:
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.
License type:
http://creativecommons.org/licenses/by-nc-nd/4.0/
Funding Info:
This work was funded by the National University of Singapore and the Agency for Science Technology and Research (A*STAR) (JCO-10/03/FG/06/02).