FRUCTIGENINE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND ANTI-INFLAMMATORY COMPOSITION CONTAINING THEM

摘要

PURPOSE: Fructigenine A derivatives, a pharmaceutically acceptable salt thereof and an anti-inflammatory composite ion containing the same are provided which can be used for treating inflammation effectively. CONSTITUTION: Fructigenine A derivatives of formula(1) as indole alkaloid prepared from strains of Penicillium sp. CJ-73 producing an anti-inflammatory substance and a pharmaceutically acceptable salt thereof and an anti-inflammatory composite ion containing the same useful as a medicament for the treatment of inflammation are described. In formula, R1 is C2-C4 alkenyl or C1-C4 alkyl, R2 is H, substituted or non substituted C1-C4 alkyl, -COCH2R6(R6 is H, C1-C6 alkyl, cyclo C3-C6 alkyl, heteroarylalkyl, substituted or non substituted phenyl or heteroaryl) or -COCHR7R8(R7R8 are the same or different H, C1-C4 alkyl, cyclo C3-C6 alkyl, heteroarylalkyl, substituted or non substituted phenyl or heteroaryl), R3 is H or C1-C4 alkyl, R4 and R5 are the same or different H or substituted or non substituted C1-C4 alkyl, aryl or benzyl. The compound has one and a half times or more the anti-inflammatory effect of indomathacin as a conventional anti-inflammatory agent by dropsy experimentation on mice.