申请人:TAISHO PHARMACEUTICAL CO. LTD
公开号:EP0113996A2
公开(公告)日:1984-07-25
Novel peptide derivatives useful as substrate for assay of EC 3.4.22 enzymes, for example, cathepsin L, cathepsin B and cathepsin H, contain an L-methionine radical and are of the formula (I)
wherein R1 represents an aliphatic acyl group containing 2-5 carbon atoms which is substituted with one or two methyl, amino, carboxyl hydroxy or benzyloxy groups, a tertiary butoxycarbonyl group or an aminobenzoyl group; or a hydrogen atom; R2 represents a 2-methylpropyl, 1-methylpropyl, p-hydroxybenzyl, p-methoxybenzyl, benzyl or 3-guanidylpropyl group; and R3 represents a naphthyl, methylcoumaryl or nitrophenyl group; or an acid addition salt thereof.
新型多肽衍生物可作为 EC 3.4.22 酶(例如 cathepsin L、chepsin B 和 cathepsin H)的底物,含有一个 L-蛋氨酸基,其结构式为 (I)
其中 R1 代表含有 2-5 个碳原子的脂肪酰基,该酰基被一个或两个甲基、氨基、羧基羟基或苄氧基、叔丁氧基羰基或氨基苯甲酰基取代;或氢原子;R2 代表 2-甲基丙基、1-甲基丙基、对羟基苄基、对甲氧基苄基、苄基或 3-胍基丙基;R3 代表萘基、甲基迷迭香基或硝基苯基;或其酸加成盐。