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pubmed-article:9873523pubmed:abstractTextA 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.lld:pubmed
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pubmed-article:9873523pubmed:affiliationDepartment of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.lld:pubmed
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