| 摘要 |
<p>Compounds of the general formula
<Chemistry id="chema01" num="0001"><Image id="ia01" he="19" wi="82" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein Ph is a phenyi group which is optionally substituted by one or more substituents selected from halo (ie fluoro, chloro, bromo or iodo), C<Sub>1-4</Sub>alkyl, amino, C<Sub>1-4</Sub>alkylamino, di-C<Sub>1-4</Sub> alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C<Sub>1-4</Sub>alkoxycarbonyl, amido, C<Sub>1-4</Sub>alkylamido, C<Sub>1-4</Sub>alkoxy, C<Sub>2-4</Sub>alkenyl, cyano, aminomethyl, or methylsulphonyl;
<UnorderedLists id="ula01" listStyle="none"><ListItem>Y is a group of formula
<Chemistry id="chema02" num="0002"><Image id="ia02" he="25" wi="83" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>where R<Sup>1</Sup> is hydrogen or methyl;</ListItem><ListItem>R<Sup>2</Sup> is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is -OR<Sup>3</Sup> or -NR<Sup>4</Sup>R<Sup>5</Sup> where R<Sup>3</Sup>, R<Sup>4</Sup> and R<Sup>5</Sup> are each hydrogen or alkyl of 1 to 4 carbon atoms and R<Sup>3</Sup> can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, eg. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkehalin analogues.</ListItem></UnorderedLists></p> |
