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桥连儿茶酚-同型半胱氨酸衍生物作为儿茶酚-O-甲基转移酶潜在抑制剂的合成

Synthesis of bridged catechol-homocysteine derivatives as potential inhibitors of catechol O-methyltransferase.

作者信息

Lever O W, Hyman C, White H L

出版信息

J Pharm Sci. 1984 Sep;73(9):1241-4. doi: 10.1002/jps.2600730912.

DOI:10.1002/jps.2600730912
PMID:6491941
Abstract

Catechol derivatives, covalently joined to homocysteine by sulfide or sulfonium linkages, were synthesized as potential catechol O-methyltransferase multisubstrate inhibitors which might bridge the enzymatic binding sites for the catechol substrate and the amino acid portion of the methyl donor S-adenosylmethionine. These compounds were found to be less effective inhibitors than the product inhibitor S-adenosylhomocysteine.

摘要

通过硫化物或锍键与同型半胱氨酸共价连接的儿茶酚衍生物被合成为潜在的儿茶酚-O-甲基转移酶多底物抑制剂，这类抑制剂可能连接儿茶酚底物的酶结合位点和甲基供体S-腺苷甲硫氨酸的氨基酸部分。结果发现，这些化合物作为抑制剂的效果不如产物抑制剂S-腺苷高半胱氨酸。

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