A novel class of enkephalinase inhibitors containing a C-terminal sulfo group

…, Y Nakamura, J Nishino, T Sawayama…

文献索引：Mimura; Nakamura; Nishino; Sawayama; Komiya; Deguchi; Kita; Matsumoto Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 602 - 608

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被引用次数: 16

摘要

A new series of sulfonic acids were synthesized and tested for their enkephalinase inhibitory activity. Among them, the most potent was N-(2-benzyl-3-mercaptopropionyl) metanilic acid 1Oi with an ICw value of 0.27 nM. Several other analogues (lOa, b, j, n, o, gg, hh) showed the inhibitory activity comparable to or greater than thiorphan (ICw= 2.6 nM), a C-terminal carboxyl-containing inhibitor of enkephalinase. Thus compounds containing a C-terminal ...