1 0 0 0 OA ペントアンスレン型構造を有する複素環化合物のモノアミン酸化酵素阻害活性
- 著者
- 野田 敦子 野田 浩司 今村 孝史 小野 行雄 森田 美華 甲斐 麻美子 嶺 佐知子 後藤 茂
- 出版者
- 公益社団法人 日本薬学会
- 雑誌
- YAKUGAKU ZASSHI (ISSN:00316903)
- 巻号頁・発行日
- vol.111, no.9, pp.499-503, 1991-09-25 (Released:2008-05-30)
- 参考文献数
- 16
- 被引用文献数
- 3 6
Pentanthrene type heterocyclic compounds, which contain oxazole, isoxazole, oxadiazole, thiazole, isothiazole, thiadiazole or pyrrole ring as C-ring, and naphthalene, quinoline, isoquinoline or quinoxaline ring as A·B-ring, were prepared, and their monoamine oxidase (MAO) inhibitory activities were examined. As expected from our previous investigation on the structure-activity relationship of this series, most of them showed strong inhibitory potency to both MAO-A and MAO-B. However, a few indicated highly selective inhibition for either of MAO subtypes.
- 著者
- 甲斐 麻美子 野田 敦子 野田 浩司 後藤 茂
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.36, no.9, pp.3604-3608, 1988-09-25 (Released:2008-03-31)
- 参考文献数
- 17
- 被引用文献数
- 8 11
This study was undertaken to evaluate the relationship between the structure and monoamine oxidase (MAO) inhibitory activity of a new series of tricyclic compounds, represented by tetrazolo-[5, 1-a]phthalazine (Tetra-P), which are based on the pentanthrene skeleton (Fig. 1.). Eleven tricyclic compounds analogous to Tetra-P were synthesized and tested as MAO inhibitors in vitro. Some of them, 1, 2, 3-triazolo[1, 5-a]quinoline (Tri-Q), tetrazolo[5, 1-a]isoquinoline (Tetra-I), 1, 2, 3-triazolo-[5, 1-a]isoquinoline (Tri-I2) and 1H-naphtho[1, 2-d]triazole (Tri-N), were found to have potent MAO inhibitory effects almost equal to that of iproniazid or nialamide. In this series of compounds, the addition of the C ring to the bicyclic skeleton seemed to produce an increase in MAO inhibitory potency compared with the corresponding bicyclic compounds. The sequence of nitrogen atoms of the C ring appeared to be important for the MAO inhibitory effect. It was concluded that the electronic conditions around the C ring are critical for the interaction between MAO and these inhibitors.
- 著者
- 甲斐 麻美子 野田 敦子 野田 浩司 後藤 茂
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.33, no.12, pp.5585-5588, 1985-12-25 (Released:2008-03-31)
- 参考文献数
- 6
- 被引用文献数
- 5 6
A new series of monoamine oxidase (MAO) inhibitors structurally analogous to tetrazolo [5, 1-a] phthalazine (Tetra-P) was detected using rat brain mitochondrial MAO. In the tricyclic group, naphtetrazole (NTE) indicated a marked potency of MAO inhibition almost equal to that of iproniazid, and naphtriazole (NTR) showed similar potency as did Tetra-P. The nonselective and competitive inhibition for both types, MAO-A and MAO-B, was observed in some Tetra-P analogues.