New immunosuppressive and antiinflammatory FR520 derivs. - for treating e.g. transplant resistance, rheumatoid arthritis, etc. are prepd. by acetylating 20,24,33-tri:hydroxy cpds.

摘要

New 19,22-furano derivs. of FR520 of formula (I) are new: where R2 = Me, Et, n-propyl or allyl; R3 = OH or OMe; and Ac = acetyl. (I) are made by conventional acylation of the 20,24,33-trihydroxy cpds.. Reaction is e.g. in pyridine, opt. in the presence of 4-dimethylaminopyridine (A), using acetic anhydride. USE/ADVANTAGE - (I) have immunosuppressive, antiinflammatory and antiproliferative activities and so can be used to treat e.g. transplant rejection; rheumatoid arthritis; multiple sclerosis; diabetes; dermatitis; acne etc.. They can be admin. topically (at a concn. of 1-3%) or systemically at 0.15-1.5 mg/kg/day. (I) also increase the activity, effect and/or sensitivity of other chemotherapeutic agents, e.g. to reduce the normal dose of toxic antineoplastic and cytostatic agents.