4.5 Article

Synthesis and biological evaluation of platensimycin analogs

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 6, Pages 1623-1627

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.006

Keywords

Platensimycin; Platensimycin analogs; FabF; Inhibition of bacterial type II fatty-acid synthesis

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Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could potentially lead to a breakthrough in developing a new generation of antibiotics. The medicinal chemistry efforts were focused on the modi. cation of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity. (C) 2009 Published by Elsevier Ltd.

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