Alkyl ether analogs of the FK-506 related, immunosuppressive macrolide L-683,590 (ascomycin)

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

C32-O-Ether derivatives of L683.590 have been prepared by alkylation with various alkyl, alkenyl, and alkynyl 2,2,2-trichloroacetimidates. These analogs exhibit good immunosuppressive activity in vitro, as measured in a T cell proliferation assay. In the case of cinnamyl ethers, this activity correlates with the lipophilicity (π value) of the aromatic substituents.

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