| 摘要 |
<p>PURPOSE:To obtain a new sulfonamide derivative exhibiting strong inhibiting action against cysteine protease such as calpain, cathepsin B, cathepsin H, cathepsin L and papain. CONSTITUTION:A sulfonamide derivative expressed by the formula I (R is 6-14C aryl or heterocyclic residue which may have one or more substituents) or its salt, e.g. N-phenylsulfonyl-L-leucine-L-valine-methyl ester. The compound of the formula I can be produced e.g. by reacting leucylvaline-methyl ester of the formula II with sulfonyl chloride of the formula III in the presence of a base, reducing the obtained ester compound of the formula IV with a reducing agent to obtain an alcohol of the formula V and oxidizing the alcohol. The compound of the formula I is useful for the treatment of diseases caused by abnormal activation of cysteine protease.</p> |
