2. Academic Validation
  3. Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acid

Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acid

  • Med Chem Res. 2018;27(3):884-889. doi: 10.1007/s00044-017-2110-8.
Alex G Baldwin 1,  Jonathan Bevan 1,  David Brough 2,  Ruth Ledder 1,  Sally Freeman 1
Affiliations

Affiliations

  • 1 1Division of Pharmacy and Optometry, School of Health Sciences, Faculty of Biology, Medicine and Health, Manchester Academic Health Science Centre, The University of Manchester, Stopford Building, Oxford Road, Manchester, M13 9PT UK.
  • 2 2Division of Neuroscience and Experimental Psychology, School of Biological Sciences, Faculty of Biology, Medicine and Health, Manchester Academic Health Science Centre, The University of Manchester, AV Hill Building, Oxford Road, Manchester, M13 9PT UK.
PMID: 29527108 DOI: 10.1007/s00044-017-2110-8
Abstract

Dehydroacetic acid is a common pyrone derivative used commercially as an Antibacterial and Antifungal agent. Based on the synthesis of dehydroacetic acid (1) from N-hydroxysuccinimdyl acetoacetate, a novel series of enamine-based derivatives were synthesised in order to improve the Antibacterial activity of dehydroacetic acid. The Antibacterial activities of the synthesised analogues were evaluated against Escherichia coli and Staphylococcus aureus. Derivative 4d (N-Ph) was identified as the most potent inhibitor of S. aureus growth. Overall, derivative 4b (N-Me) showed the best broad-spectrum activity with five-fold greater minimum inhibitory concentration and 11-fold greater minimum biocidal concentration against E. coli when compared to dehydroacetic acid, in addition to improved Antibacterial activity against S. aureus.

Keywords

Antibacterial activity; Dehydroacetic acid; Pyran-2, 4-diones; SAR; Staphylococcus aureus.

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