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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Bibliographic Details
Published in:Bioconjugate chemistry 1992-01, Vol.3 (1), p.32-36
Main Authors: Paprica, P. A., Margaritis, A., Petersen, N. O.
Format: Article
Language:English
Subjects:
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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Summary: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