9A-N-(N'-CARBAMOYL) AND 9A-N-(N'-THIOCARBAMOYL) DERIVATIVES OF 9-DEOXO-9A-AZA-9A-HOMOERYTHROMYCIN A, PROCESS FOR THEIR PREPARATION, PHARMACEUTICALS AND USE THEREOF

摘要

The invention relates to novel semisynthetic macrolide antibiotics of the azalide series, of the formula (I) wherein R represents a C1-C3 alkyl, aryl or aralkyl group and X represents O or S, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids. Also disclosed is a process for preparing the se derivatives by reacting 9-deoxo-9a-aza-9a-homoerythromycin A and isocyanates or isothiocyanates in a solvent at a temperature of 20 to 110 DEG C. A pharmaceutical composition contains 9a-N-(N'-carbamoyl) and 9a-N-(N'-thiocarbamoyl) derivatives of 9-deoxo-9a- -aza-9a-homoerythromycin A as an antibacterial agent together with a pharmaceutically acceptable carrier and is useful in treating bacterial infections.