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The synthesis and antibacterial activity of totarol derivatives. part 1: modifications of ring-C and pro-drugs by Gary B Evans; Richard H Furneaux; Michael B Gravestock; Gregory P Lynch; G.Kenneth Scott is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is The synthesis and antibacterial activity of totarol derivatives. part 1: modifications of ring-C and pro-drugs about?
AbstractÐA series of analogues of, and potential pro-drugs derived from, the potent antibacterial diterpene totarol (1) were synthesized in order to elucidate the minimum structural requirements for antibacterial activity and to seek compounds with good bioavailability in vivo. These analogues varied in the structural features of their aromatic rings and the prodrugs were O-glycosylated derivatives. They were tested in vitro against three Gram-positive bacteria: b-lactamase-positive and high level gentamycinresistant Enterococcus faecalis, penicillin-resistant Streptococcus pneumoniae, and methicillin-resistant Staphylococcus aureus (MRSA); and against the Gram-negative multi-drug-resistant Klebsiella pneumoniae. None of the analogues was more potent than totarol itself, which is eective against these Gram-positive bacteria at MIC values of 7 mM. The results were evaluated in terms of a structure±activity relationship and this showed that a phenolic moiety was essential for potent antibacterial activity. Amongst the pro-drugs, totaryl a-d-mannopyranoside (22) proved the most active in vitro (MIC 18 mM). The in vivo antibacterial activities of compounds 1, 22 and totarol b-lactoside
Who reads The synthesis and antibacterial activity of totarol derivatives. part 1: modifications of ring-C and pro-drugs?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Gary B Evans; Richard H Furneaux; Michael B Gravestock; Gregory P Lynch; G.Kenneth Scott
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 1999
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)