The synthesis and antibacterial activity of totarol derivatives. Part 3: modification of ring-B
Ring-B derivatization of totarol (1) afforded the series of compounds 2-22 which were screened in vitro against: β-lactamase-positive and high level gentamycin-resistant Enterococcus faecalis, penicillin-resistant Streptococcus pneumoniae, methicillin-resistant Staphylococcus aureus (MRSA), and multiresistant Klebsiella pneumoniae. Several of the derivatives retained much of the antibacterial activity of totatol against the first three of these organisms (all Gram-positive), but none was more active. The Gram-negative Klebsiella was resistant to all compounds examined. Totarol (1) was shown to uncouple oxidative phosphorylation in isolated mitochondria at 50 μM. Copyright (C) 2000 Elsevier Science Ltd.
Evans, Gary B.,Furneaux, Richard H.,Gainsford, Graeme J.,Murphy, Michael P.
p. 1663 - 1675
(2007/10/03)
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