| 摘要 |
3-Descladinose-2,3-anhydroerythromycin derivatives e.g. of formulae (I) and (II) and their salts and esters are new. q = 0 or 1; Q1 = a group of formula (i); R1 = H, OH, 1-12C alkoxy, OCO-(1-6C)alkyl, OCONH2, OCONHCO-(1-12C)alkyl or OCONHSO2-(1-12C)alkyl; R2 = H or hydroxy protecting group; R = H, 1-6C alkyl (optionally substituted by Ar, Het, OH, 1-6C alkoxy, NR3R4 or CH2MR5), 3-7C cycloalkyl, Ar or Het; Ar = optionally substituted aryl; Het = optionally substituted heteroaryl; R3, R4 = H or 1-6C alkyl; or NR3R4 = 3-7 membered ring optionally containing O, NH, N(1-6C alkyl ), N(aryl), N(Ar-1-6C alkyl), N(Het 1-6C alkyl) or S(O)n when the ring is 5-7 membered; n = 0-2; M= CONH, NHCO, NH, N=, N(Me), O, S(O)n, COO, OCO or CO; R5 = 1-6C alkyl (optionally substituted by Ar or Het), Ar, Het or heterocycloalkyl; W = absent, O, NHCO, N=CH, NH or N(1-6C alkyl); A, B, D, E = (i) H, 3-7C cycloalkyl, Ar, Het or heterocycloalkyl or (ii) 1-6C alkyl optionally substituted by one or more Ar, Het, heterocycloalkyl, 1-6C alkoxy, halo or NR3R4 all (ii) optionally further substituted by MR5; or 2 of A, B, D and E complete 3-7 membered ring optionally containing O, NH, N(1-6C alkyl), N(Ar-1-6C alkyl), N(Het-1-6C alkyl), S(O)n, CONH, CONR5, NHCO, NR5CO or C(=NH)NH. #CMT#USE : #/CMT# (I) are antibacterial agents. Dosage is e.g. 0.01-50 (preferably 0.1-25) mg/kg/day. |
