Precursor-directed syntheses and biological evaluation of new elansolid derivatives

Date

2012-8

Type

Article

Journal title

Chembiochem

Issue

Vol. 12 No. 13

Author(s)

Heinrich Steinmetz
Wiebke Zander
Muftah A. M. Shushni
Rolf Jansen
Klaus Gerth
Richard Dehn
Gerald Dräger
Andreas Kirschning
Rolf Müller

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. arabic 9 English 74

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