title: New oleandomycin 9-oximes. Synthesis, characterization and biological activity.
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.
authors.affiliation: PLIV--Pharmaceutical, Chemical, Food and Cosmetic Industry, Research Institute, Zagreb, Croatia.
authors.forename: G
authors.initials: G
authors.lastname: Lazarevski
authors.forename: G
authors.initials: G
authors.lastname: Kobrehel
authors.forename: S
authors.initials: S
authors.lastname: Dokić
authors.forename: L
authors.initials: L
authors.lastname: Kolacny-Babić
authors.forename: B
authors.initials: B
authors.lastname: Kojić-Prodić
authors.forename: D
authors.initials: D
authors.lastname: Janković
authors.forename: V
authors.initials: V
authors.lastname: Puntarec
mesh_terms: D000818:Animals; D001419:Bacteria / Q000187:drug effects; D003461:Crystallography; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009827:Oleandomycin / Q000031:analogs & derivatives / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D014018:Tissue Distribution
chemical_list: D009827:Oleandomycin