| Research Abstract |
According to the structure - MAO inhibitory activity relationship of tricyclic compounds which contain a pentanthrene skeleton,it was clarified that electronic condition around the C-ring seemed to be critical for the interaction between MAO and the inhibitors. Based on the observation, a lot of pentanthrene type compounds which include some of Nitrogen atoms,Oxygen atoms,Sulfur atoms and/or methyl group in the C-ring were designed and synthesized. Most of them showed the strong MAO inhibitory potency like iproniazid. A few of them indicated a selective inhibition to MAO-B.It is an important result for the development of a therapeutic agent for perkinsonism. Furthermore,some anxiolytic activities were newly detected in the series of pentanthrene type heterocycles. Therefore,the fates of some compounds which show the MAO inhibition and/or anxiolytic activity were also examined using rabbits and rats.
In the study mentioned above,many valuable observations for the development of the therapeutic drugs were obtained especially for the detection of a few of biological activities in a similar series of pentanthrene type heterocycles.
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