Precursor-directed syntheses and biological evaluation of new elansolid derivatives |
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| Authors: | Heinrich Steinmetz Wiebke Zander Muftah A M Shushni Rolf Jansen Klaus Gerth Richard Dehn Gerald Dräger Andreas Kirschning Rolf Müller |
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| Affiliation: | Helmholtz Centre for Infection Research, Research Group Microbial Drugs, Inhoffenstrasse 7, 38124 Braunschweig (Germany). |
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| Abstract: | The antibiotic elansolid C1 (8) was isolated from Chitinophaga sancti strain FxGBF13 after fermentation in the presence of anthranilic acid. Remarkably, 8 was also obtained by addition of anthranilic acid to a crude fermentation extract containing the macrolide elansolid A2 (1*). This Michael-type conjugate addition allowed us to generate 21 new derivatives of elansolid C1 (9-29) by using various nucleophiles. Biological activities of all derivatives were evaluated against Staphylococcus aureus, Micrococcus luteus, and the mouse cell line L929. |
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| Keywords: | anthranilic acid antibiotics elansolid liquid chromatography nucleophiles |
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