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.; Suwanarusk, R.; Ngai, M.H.; Srinivasan, R.; Ong, A.S.M.; Ho, B.; Rénia, L.; Chai, C.L.L.

Bioorganic and Medicinal Chemistry Letters 25(3): 607-610


ISSN/ISBN: 1464-3405
PMID: 25544370
DOI: 10.1016/j.bmcl.2014.12.014
Accession: 057176773

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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.