| 摘要 |
<p>Novel beta -lactams of the general formula (1) are disclosed: <IMAGE> wherein: R1 represents an aliphatic acyl or alkoxycarbonyl group or the aminocarbonyl group, and X represents the group <IMAGE> wherein D represents an hydrogen atom; an acetoxy; aminocarbonyloxy; pyridinium; or 4-aminocarbonyl-pyridinium group; or a group -SHet (Het represents, for example, the 1-methyl-tetrazole-5-yl radical), and E represents an hydrogen atom or an in vitro or in vivo readily cleavable protective group, and R represents an hydrogen atom; the cyclopropyl group; a lower hydroxyalkylamino group; an amino; alkyl; or alkenylamino group; a cycloalkylamino group; or a group of the general formula: <IMAGE> wherein n represents the number 0 or 1, and R3 and R4 represent hydrogen atoms; hydroxy; acetylamino; aminocarbonylamino; nitro; aminocarbonyl; cyano; methylsulfinyl; methylsulfonyl; aminosulfonyl; or methylaminosulfonyl groups. Salts of the compounds (I) with inorganic or organic bases, 3 processes for the preparation of these compounds and pharmaceutical compositions containing these compounds are also described. The compounds of the general formula (I) have additionally an activity against gram-positive and especially against gram-negative bacteria and micro-organisms similar to bacteria; the compounds being distinguished especially by a broad spectrum of activity.</p> |
