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 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.
Paprica
P A
PA
Department of Chemistry, University of Western Ontario, London, Canada.
Margaritis
A
A
Petersen
N O
NO
D002855:Chromatography, Thin Layer; D003524:Cyclosporins / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy
D003524:Cyclosporins