| 摘要 |
EP--90656 A N-Heterocyclyl-carbonylampicillin derivs. and analogues of formula (I) and their salts and in vitro hydrolysable esters are new. - R1 is opt. substd. Ph or a 5- or 6-membered heterocyclic ring contg. up to 3 N, O or S and opt. substd. by OH, NH2, halogen or 1-6C alkoxy; X is heterocyclic gp. of formula (IIa), (IIb) and (IIc); R1 is Me or MeCO; R2 and R3 are H, aryl, heterocyclyl or 1-6C alkyl opt. substd. by an aryl gp. or a heterocyclyl gp.; R4 is H, 1-6C alkanoyl aryl, heterocyclyl, 1-6C alkyl opt. substd. by an aryl gp. or a heterocyclyl gp.; R5 is H, MeO or NH-CHO; Y is -S-CMe2-, -S-CH2- or -Y1-CH2-CZ:; Y1 is O, S or CH2; Z is H, halogen or an organic gp., esp. 1-4C alkoxy, CH2Q or CH:CHQ; and Q is H halogen, OH, SH, CN, COOH, carbamoyloxy carboxylic ester, 1-4C alkoxy, acyloxy, aryl, heterocyclyl (bonded via a C atom) heterocyclylthio or N-contg. heterocyclyl (bonded via N atom). - Cpds. (I) are broad-spectrum antibacterials esp. useful for treating respiratory tract and urinary tract infections in man and mastitis in cattle. (0/0) USAB- US4537886 A Beta-lactams with pyrazolinone in acylamine side chain of formula (A) are new. In (I), R1 is Ph opt. substd. 5 or 6-membered heterocycle of up to 3 O, S or N (opt. substd. OH, NH2, halo, or 1-6Calkoxy; X is in which Ry is Me or Ac; R2 and R3 are each H 1-6C alkylcarbonyl, aryl heterocycle, 1-6C alkyl opt. substd.; R5 is H, MeO, -NHCHO, and Y is IV-VI in which Y' is O, S or CH2 and Z is H, halo, 1-4C alkoxy, -CH2Q, -CH0CH-Q with Q, H, halo, OH, SH, CN, COO, carbamoyloxy carboxylic ester, 1-4C alkoxy, acyloxy, aryl, heterocycle. (A) are prepd. by reacting cpds(B) with an N-acylating deriv. of acid X-COOH.
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