| 摘要 |
New carbapenem compounds (I). Carbapenem compounds of formula (I) are new. [Image] R 1CH 2OCOC(Me) 3, CH 2OCOOCH(Et) 2, CH(Me)OCOOCH(Et) 2 or CH 2OCOOCyc; Cyc : cyclohexyl or cyclopentyl; R 2CH 2CH 2CH 3, CH 2CH 3 or CH(Me) 3; provided that: (1) when R 1 = CH 2OCOC(Me) 3 then R 2 = CH 2CH 2CH 3; and (2) when R 1 = CH 2OCO 2Cyc then R 2 is not Et. ACTIVITY : Antibacterial. In bioavailability studies in rats administration of pivaloyloxymethyl (1R,5S,6S)-2-[(3S,5S)-(5-N,N-dimethylaminocarbonyl-1-butyryloxymethyloxycarbonyl)pyrrolidin-3-ylthio]-6-[(1R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylate (Ia) at 20 mg/kg orally gave an AUC (0-3 hours) of 5.06 mu g.hr/ml. MECHANISM OF ACTION : None given. |
