申请人:THE WELLCOME FOUNDATION LIMITED
公开号:EP0038046A2
公开(公告)日:1981-10-21
Compounds of the general formula
(wherein X is a group capable of functioning as a ligand for a zinc ion;
Ph ist a phenyl group which is optionally substituted by one or more substituents selected from halo and nitro radicals;
Y is a group of formula:
where
R' is hydrogen or methyl;
R2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and
Z is a group of formula -OR3 or -NR4R5 where R3, R4 and
R5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R' can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl) and pharmacologically acceptable basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds of use in medical therapy for example when it is desired to prolong and/or potentiate in a mammal the effects of enkephalins of either endogenous or exogenous origin including in the later case synthetic enkephalin analogues.
通式如下的化合物
(其中 X 是可用作锌离子配体的基团;
Ph 是苯基,可任选被选自卤代和硝基的一个或多个取代基取代;
Y 是式中的一个基团:
其中
R' 是氢或甲基
R2 是 1 至 3 个碳原子的烷基或甲硫基;以及
Z 是式-OR3 或-NR4R5 的基团,其中 R3、R4 和
R'还可以是在其亚烷基中含有 1 至 3 个碳原子的苯基烷基或苯基)及其药理学上可接受的碱式盐。这些化合物具有良好的脑啡肽酶抑制活性,可用于医学治疗,例如延长和/或增强哺乳动物体内内源性或外源性脑啡肽(包括合成脑啡肽类似物)的作用。