title: Preparation of novel cyclosporin A derivatives.
abstract: 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.
authors.affiliation: Department of Chemistry, University of Western Ontario, London, Canada.
authors.forename: P A
authors.initials: PA
authors.lastname: Paprica
authors.forename: A
authors.initials: A
authors.lastname: Margaritis
authors.forename: N O
authors.initials: NO
authors.lastname: Petersen
mesh_terms: D002855:Chromatography, Thin Layer; D003524:Cyclosporins / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy
chemical_list: D003524:Cyclosporins