NEW OLEANDOMYCIN 9-OXIMES SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY

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)-rriethylolea...

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Veröffentlicht in:	Journal of antibiotics 1994/03/25, Vol.47(3), pp.349-356
Hauptverfasser:	LAZAREVSKI, GORJANA, KOBREHEL, GABRIJELA, DOKIC, SLOBODAN, KOLACNY-BABIC, LIDIJA, KOJIC-PRODIC, BISERKA, JANKOVIC, DRAGAN, PUNTAREC, VITOMIR
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacteria - drug effects Biological and medical sciences Crystallography In Vitro Techniques Magnetic Resonance Spectroscopy Medical sciences Microbial Sensitivity Tests Oleandomycin - analogs & derivatives Oleandomycin - chemistry Oleandomycin - pharmacokinetics Oleandomycin - pharmacology Pharmacology. Drug treatments Rats Tissue Distribution
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Zusammenfassung:	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)-rriethyloleandomycin-9-oxime (9) in contrast to 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.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.47.349