Chemical Transformations of Antibiotic X-537A and Their Effect on Antibacterial Activity

John W. Westley, Eugene P. Oliveto, Julius Berger, Ralph H. Evans, Richard Glass, Arthur Stempel, Voldemar Toome, Thomas Williams

Research output: Contribution to journalArticle

45 Scopus citations

Abstract

A number of derivatives of the polyether antibiotic X-537A have been tested in vitro vs. Bacillus E and Bacillus TA and the results clearly indicate that all the oxygen functions involved in ligand formation with cations and intramolecular hydrogen bonding (as revealed by X-ray analysis) contribute to the biological activity of the antibiotic. In addition, a number of derivatives at the C-5 position of the aromatic chromo-phore exhibited a qualitative correlation between their partition coefficients (octanol-water) and in vitro activity.

Original languageEnglish (US)
Pages (from-to)397-403
Number of pages7
JournalJournal of Medicinal Chemistry
Volume16
Issue number4
DOIs
StatePublished - Apr 1 1973

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Westley, J. W., Oliveto, E. P., Berger, J., Evans, R. H., Glass, R., Stempel, A., Toome, V., & Williams, T. (1973). Chemical Transformations of Antibiotic X-537A and Their Effect on Antibacterial Activity. Journal of Medicinal Chemistry, 16(4), 397-403. https://doi.org/10.1021/jm00262a020