214411-64-0Relevant academic research and scientific papers
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential
Goulet, Mark T.,McAlpine, Shelli R.,Staruch, Mary Jo,Koprak, Samuel,Dumont, Francis J.,Cryan, John G.,Wiederrecht, Gregory J.,Rosa, Raymond,Wilusz, Mary Beth,Peterson, Laurence B.,Wyvratt, Matthew J.,Parsons, William H.
, p. 2253 - 2258 (1998)
A series of C32-O-aralkyl ether derivatives of the FK-506 related macrolide ascomycin have been prepared based on an earlier reported C32-O- cinnamyl ether design. In the present study, the nature of the aryl tethering group was varied in an attempt to improve oral activity. An imidazol-2-yl- methyl tether was found to be superior among those investigated and has resulted in an ascomycin analog, L-733,725, with in vivo immunosuppressive activity comparable to FK-506 but with an improved therapeutic index.
