| 摘要 |
New beta-lactam antibiotics are of formula (I) and their hydrates (where R is H or UR'; U is O or S; R' is alkyl, alkenyl aralkyl, aryl or cycloalkyl, all opt substd.; Z is R1R2C=N- or R1R2C(OH)-NH-; R1 and R2 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, aralkyl, heterocyclyl (all opt. substd.). COOH, (m)ethoxycarbonyl, CN, NO2, lower alkanoyl, or CONH2 or SO2NH2 both opt. substd. by 1 or 2 CH3; or R1R2C is an opt. satd. or unsatd. and opt. substd. 3-7 membered carbocyclic or heterocyclic ring; A is (CH2)2, (CH2)3 or 1,2-phenylene; B is opt. substd. phenyl, cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO2 or CH2; Y is -C(CH3)2, CHCOOE or -CH2.C(CH2T)=C-COOE; T is H, alkanoyloxy, pyridinium, aminopyridinium, carbamoyloxy, N3, CN, OH, opt. substd. phenylthio or -SHet; Het is opt. substd. 5 or 6 membered heterocycle; and E is H, pharmaceutically acceptable ester gp. (e.g. pivaloyl), salt-forming cation or a protecting gp.). Both R and S configurations at the asterisked C atom (and their mixts.) are included, and when R1 is not =R2 in R1R2C=N-, the configuration can be syn or anti. (I) are antibacterials useful for treating infections; for increasing growth rate and feed utilisation in animals and for preserving goods such as polymers, lubricants, paper etc. They have a broader spectrum of activity than known antibiotics esp. against several Gram neg. families. |
