| 摘要 |
Clavamic acid derivatives of the formula <IMAGE> in which R is -NH2 and R<3> is -COOH or an esterified carboxyl group, are prepared from corresponding azides, R = -N3 in the above formula, by reduction. The free carboxylic acid can be in the form of a zwitterion or a salt with acids or bases; it can be esterified. The starting material with R = -N3 is advantageously prepared from an ester of the formula II in which R is an exchangeable atom or an exchangeable group by reaction with an azide. The products (II), especially the free carboxylic acid, have antibacterial activity on various Gram-negative and Gram-positive microorganisms and they inhibit beta -lactamase; they can be used alone as antibiotics or in combination with beta -lactam antibiotics for the treatment of infectious diseases. |
