Preparation of novel cyclosporin A derivatives

The hydroxyl group on the 2-N-methyl-(R)-((E)-2-butenyl)-4-methyl-L-threonine residue of cyclosporin A was protected by acetylation, then the double bond on the same amino acid residue was oxidatively cleaved using a periodate/permanganate reagent. The resultant derivative of cyclosporin A contained...

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Veröffentlicht in:	Bioconjugate chemistry 1992-01, Vol.3 (1), p.32-36
Hauptverfasser:	Paprica, P. A., Margaritis, A., Petersen, N. O.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Biotechnology Chromatography, Thin Layer Cyclosporins - chemical synthesis Cyclosporins - chemistry Fundamental and applied biological sciences. Psychology Health. Pharmaceutical industry Industrial applications and implications. Economical aspects Magnetic Resonance Spectroscopy
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Beschreibung
Zusammenfassung:	The hydroxyl group on the 2-N-methyl-(R)-((E)-2-butenyl)-4-methyl-L-threonine residue of cyclosporin A was protected by acetylation, then the double bond on the same amino acid residue was oxidatively cleaved using a periodate/permanganate reagent. The resultant derivative of cyclosporin A contained a carboxylic acid group which was subsequently reacted with the nucleophiles 5-(aminoacetamido)fluorescein and poly(L-lysine), in the presence of 1-ethyl-3-[3-(dimethylamino)propyl] carbodiimide, to furnish novel cyclosporin A conjugates.
ISSN:	1043-1802 1520-4812
DOI:	10.1021/bc00013a005