1992 Fiscal Year Final Research Report Summary
The primary study for the development of CNS-related drugs -Especially for a therapeutic agent of Perkinsonism-
| Project/Area Number |
03671056
|
|---|
| Research Category |
Grant-in-Aid for General Scientific Research (C)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
Biological pharmacy
|
|---|
| Research Institution | KYUSHU UNIVERSITY |
|---|
Principal Investigator |
NODA Atsuko Kyushu University,Dept.of Pharmaceutical Sciences Associate Professor, 薬学部, 助教授 (00037582)
|
|---|
| Project Period (FY) |
1991 – 1992
|
| Keywords | CNS-related drugs / Pentanthrene type heterocycles / QSAR analyses / Drug design / MAO inhibitor / Antidepressant / Anxiolytics / Drug behavior |
|---|
| 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.
|
