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

R Hersperger, W Schuler, G Zenke

Index: Hersperger, Rene; Schuler, Walter; Zenke, Gerhard Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 2 p. 227 - 232

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Citation Number: 8

Abstract

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.