Derivatives of macrolide antibiotics.

摘要

Compounds of the following general formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="63" wi="103" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>R<Sup>1</Sup> and R<Sup>2</Sup> represent a hydrogen atom or a lower alkanoyl group:</ListItem><ListItem>R<Sup>3</Sup> represents a hydrogen atom or the group -COCH<Sub>2</Sub>R<Sup>5</Sup> in <!-- EPO <DP n="2"> -->which R<Sup>5</Sup> represents a lower alkyl group or an aryl or pyridyl group bonded through a sulfur atom;</ListItem><ListItem>R<Sup>4</Sup> represents a methyl group which may be substituted by aryl, pyridyl, pyridylthio, hydroxyl or arylthioamino, an aryl group, a nitrile group, a 5- or 6-membered heterocyclic group having 1 to 4 hetero atoms selected from nitrogen and sulfur atoms, or a tetra-hydropyranyl group which may be substituted by methoxy;</ListItem><ListItem>A represents the group -OCO-, -OS0<Sub>2</Sub>-, -O- or -S-, or A and R<Sup>4</Sup>, taken together, represent a halogen atom, a nitrile group or a group of the formula -NR<Sup>6</Sup> in which R<Sup>6</Sup> represents two lower alkyl groups, the group
<Chemistry id="chema02" num="0002"><Image id="ia02" he="30" wi="39" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>or an alkylene group having 4 to 6 carbon atoms which may have in the chain an oxygen atom or a lower alkyl-substituted nitrogen atom; and said aryl group and heterocyclic group may optionally be substituted by a methyl, methoxy or nitro group, and when R<Sup>1</Sup> represents a lower alkyl group, R<Sup>3</Sup> does not represent a lower alkyl group or their salts.</ListItem></UnorderedLists>

These novel derivatives of macrolide antibiotics have excellent antibacterial activity.