Amphotericin B Dimers with Bisamide Linkage Bearing Powerful Membrane-Permeabilizing Activity
(Matrix Presented) Covalently linked dimers of amphotericin B were prepared by cross-linking its carboxylic acid. Among these, a dimer with a linkage of 1,6-hexanediamine revealed potent hemolytic activity (EC50,0.25 μM) while its N-acetyl deri
Retrosynthetic and Synthetic Chemistry on Amphotericin B. Synthesis of C(1)-C(20) and C(21)-C(38) Fragments and Construction of the 38-Membered Macrocycle
For the first time, amphotericin B (I) has been successfully derivatized and degraded to intermediates that have been converted into compounds (II) and (III) , projected as major key intermediates for a total synthesis; methods have been developed for the coupling of fragments (II) and (III) to give the ketophosphonate-aldehyde (28) and for the cyclization of this precursor to the 38-membered macrocyclic heptaenone (29) in 70-80percent yield.
Nicolaou, K. C.,Chakraborty, T. K.,Daines, R. A.,Simpkins, N. S.
p. 413 - 416
(2007/10/02)
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