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Synthesis and structure-activity relationship of antifungal coniothyriomycin analogues
Karsten Krohn1, Brigitta Elsässer, Sándor Antus
1Department of Chemistry, University of Paderborn, Warburger Strasse 100, 33098 Paderborn, Germany. kk@chemie.uni-paderborn.de
The Journal of Antibiotics
|May 23, 2003
Abstract:
The structure of the antifungal metabolite coniothyriomycin was systematically modified by changing the acids of the open chain imide, modification of the hydrophobicity, variation in the degree of saturation, replacement of carbons by nitrogen or oxygen, and incorporation of the open chain molecule into cyclic arrangements. Structure-activity studies showed that antifungal activity was retained by replacement of phenylacetic acids by benzoic acids in the imide structure but diminished by hydrogenation of the fumaric ester part.