| 摘要 |
There are provided 3-azinomethyl rifamycins of the formula I: <IMAGE> (I) wherein R represents hydrogen or acetyl; R1 represents hydrogen or lower alkyl; R2 represents an alkyl group having from 2 to 4 carbon atoms substituted by a dialkoxy group each having from 1 to 3 carbon atoms; R3 represents an alkyl group having from 1 to 4 carbon atoms; R2 and R3 may form with the amino nitrogen atom a 4- to 8-membered heterocyclic ring, having a maximum of two hetero atoms, substituted by hydroxy-, alkoxy-, dialkoxy- or alkylenedioxy groups each having from 1 to 4 carbon atoms, arylalkoxyimino groups having from 7 to 9 carbon atoms, acyloxy groups having from 1 to 4 carbon atoms; R1 and R2 may form with the amino nitrogen atom and the carbon atom a 5 to 7-membered heterocyclic ring optionally substituted by alkyl or alkoxy group having from 1 to 4 carbon atoms. The compounds display antibacteria activity against Gram-positive and Gram-negative bacteria and Mycobacteria. Process for the preparation of the above compounds and their pharmaceutical compositions are also described and claimed. |
