| abstract |
Derivatives of pleuromutilin of formula (IA) or (IB) in which the glycolic ester moiety at position (14) is replaced by R2(CH2)mX(CH2)nCH2COO are of use in antimicrobial therapy. In which: each of n and m is independently 0, 1 or 2; X is selected from -O-, -S-, S(O)-, -SO2-, -CO.O-, -NH-, -CONH-, NHCONH- and a bond; R1 is vinyl or ethyl; R2 is a non-aromatic a monocyclic or bicyclic group containing one or two basic nitrogen atoms and attached through a ring carbon atom; R3 is H or OH; or the moiety R2(CH2)mX(CH2)nCH2COO at position 14 of (IA) or (IB) is replaced by RaRbC=CHCOO in which one of R?a and Rb¿ is hydrogen and the other is R?2 or Ra and Rb¿ together form R2; or a pharmaceutically acceptable salt thereof. |