Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acidCitation formats

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Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acid. / Freeman, Sally; Ledder, Ruth.

In: Medicinal Chemistry Research, 03.2018.

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@article{76aa7145b57048f69058b3accedea1a7,
title = "Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acid",
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",
author = "Sally Freeman and Ruth Ledder",
year = "2018",
month = "3",
doi = "10.1007/s00044-017-2110-8",
language = "English",
journal = "Medicinal Chemistry Research",
issn = "1054-2523",
publisher = "Birkh{\"a}user Boston",

}

RIS

TY - JOUR

T1 - Synthesis and antibacterial activities of enamine derivatives of dehydroacetic acid

AU - Freeman, Sally

AU - Ledder, Ruth

PY - 2018/3

Y1 - 2018/3

N2 - 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

AB - 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

U2 - 10.1007/s00044-017-2110-8

DO - 10.1007/s00044-017-2110-8

M3 - Article

JO - Medicinal Chemistry Research

JF - Medicinal Chemistry Research

SN - 1054-2523

M1 - DOI10.1007/s00044-017-2110-8

ER -