Preparation and immunosuppressive activity of 32-(O)-acylated and 32- (O)-thioacylated analogues of ascomycin

Article abstract of DOI:10.1016/S0960-894X(98)00702-1

A series of 32-(O)-acylated and 32-(O)-thioacylated derivatives of the antibiotic ascomycin (1) have been synthesized. These readily accessible analogues exhibit potent immunosuppressive activity in vitro, as measured by an interleukin-2 reporter gene assay and the mixed lymphocyte reaction. Such molecules are expected to have a therapeutic potential in chronic inflammatory diseases of the airways such as asthma.