In:
Biotechnology and Applied Biochemistry, Wiley, Vol. 59, No. 4 ( 2012-07), p. 295-306
Abstract:
Seven novel β‐lactam antibiotics with activities against Gram‐positive bacterial strains, among them methicillin‐resistant Staphylococcus aureus and vancomycin‐resistant enterococci, were synthesized by amination of 2,5‐dihydroxyphenylacetic acid in usable yields (30–60%). These products protected mice against an infection with S. aureus lethal to the control animals. The results show the usefulness of laccase for the synthesis of potential new antibiotics, in addition to the interdependence of the laccase substrates, the amino coupling partners, and the product formation, yield, and activity. The syntheses of β‐lactam antibiotics with 2,5‐dihydroxyaromatic acid substructures ( para ‐substituted) are then compared with those of 3,4‐dihydroxyaromatic acid substructures ( ortho ‐substituted). Para ‐substituted laccase substrates were better reaction partners in these syntheses than ortho ‐substituted compounds.
Type of Medium:
Online Resource
ISSN:
0885-4513
,
1470-8744
Language:
English
Publisher:
Wiley
Publication Date:
2012
detail.hit.zdb_id:
1496341-3
SSG:
12
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