| 摘要 |
<p>There are provided 3-azinomethyl rifamycins of the for- mulal:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="56" wi="67" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>R represents hydrogen or acetyl;</ListItem><ListItem>R<Sub>1</Sub> represents hydrogen or lower alkyl;</ListItem><ListItem>R<Sub>2</Sub> represents an alkyl group having from 2 to 4 carbon atoms substituted by a dialkoxy group each having from 1 to 3 carbon atoms;</ListItem><ListItem>R<Sub>3</Sub> represents an alkyl group having from 1 to 4 carbon atoms;</ListItem><ListItem>R<Sub>2</Sub> and R<Sub>3</Sub> 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;</ListItem><ListItem>R<Sub>1</Sub> and R<Sub>2</Sub> 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.</ListItem></UnorderedLists></p><p>The compounds display antibacteria activity against Gram-positive and Gram-negative bacteria and Mycobacteria.</p><p>Process for the preparation of the above compounds and their pharmaceutical compositions are also described and claimed.</p> |
