Curcumin derivative

摘要

The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof:;
wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.

主权项

1. A compound represented by the following general formula (I) or a salt thereof: wherein R1 represents a phenyl group which is substituted by one or more substituents independently selected from the group consisting of hydroxy and methoxy group, and R2 represents a 1H-indol-2-yl, 1H-indol-3-yl, 1H-indol-4-yl, 1H-indol-5-yl, 1H-indol-6-yl, or 1H-indol-7-yl group which may be substituted by one or two or more substituent(s) selected from a substituent group A; and the substituent group A is a group selected from the group consisting of halogen atoms, alkyl groups having 1 to 6 carbon atom(s), alkoxy groups having 1 to 6 carbon atom(s), dialkylamino groups (wherein the alkyl group has 1 to 6 carbon atom(s)), alkylamino groups (wherein the alkyl group has 1 to 6 carbon atom(s)), amino groups, alkoxyalkoxy groups having 2 to 6 carbon atoms, hydroxy groups, acetylamino groups, phenoxy groups, methanesulfonyl groups, methylthio groups, nitro groups, 3-dimethylaminopropoxy groups, 2-dimethylaminoethoxy groups, dimethylaminomethoxy groups, acetoxy groups, methoxycarbonyl groups, pyridin-2-yl groups, 1H-imidazol-1-yl groups, 4-benzylpiperazin-1-yl groups, 4-methylphenoxy groups, morpholino groups, 4-methylphenyl groups, phenyl groups, benzimidazol-1-yl groups, 4-methylpiperazin-1-yl groups, 2-(t-butoxycarbonylamino)acetylamino groups, 2-t-butoxycarbonylamino-3-phenylpropionylamino groups, benzyl groups, acetyl groups, tosyl groups, methylsulfonyloxy groups, t-butoxycarbonylamino groups, N-(t-butoxycarbonyl)-N-methylamino groups, t-butyldimethylsilyloxy groups, t-butyldimethylsilyloxymethyl groups, 2-amino-3-phenylpropionylamino groups, hydroxymethyl groups, benzoyloxy groups, prenyloxy groups, benzyloxy groups, i-propyloxy groups, 2-hydroxyethoxy groups, 2-(amino)acetylamino groups, 4-methoxybenzyloxy groups, pyridin-3-ylmethoxy groups, 2-chloro-6-fluorobenzyloxy groups, 2,4-dichlorobenzyloxy groups, 4-t-butylbenzyloxy groups, trifluoromethyl groups, hydroxycarbonyl groups, dimethylaminocarbonyl groups, dimethylaminosulfonyl groups, methylsulfinyl groups, pyrrolidin-1-yl groups, piperidin-1-yl groups, t-butoxycarbonylpiperazin-1-yl groups, methylsulfonylpiperazin-1-yl groups, 2-hydroxyethylpiperazin-1-yl groups, pyridin-3-yl groups, pyridin-4-yl groups, piperazin-3-yl groups, naphthalen-1-yl groups, and naphthalen-2-yl groups.