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New oleandomycin 9-oximes. Synthesis, characterization and biological activity
G Lazarevski1, G Kobrehel, S Dokić
1PLIV--Pharmaceutical, Chemical, Food and Cosmetic Industry, Research Institute, Zagreb, Croatia.
The Journal of Antibiotics
|March 1, 1994
Abstract:
A series of the novel oleandomycin 9-oximes has been prepared and characterized by spectroscopic data and X-ray analysis. The antibacterial in vitro activities of the oximes (6-10) were compared with that of oleandomycin (1). Among the novel derivatives the most active compound was 8(R)-methyloleandomycin-9-oxime (9) in contrast ot its 8(S)-isomer (10) which possessed only low potency. Some preliminary pharmacokinetic data of 9 confirmed its activity. Compound 9 has been advanced to further biological study.