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Inhibitors of monoamine oxidase III: 9-substituted-β-carbolines

✍ Scribed by Beng T. Ho; William M. McIsaac; L. Wayne Tansey; K. E. Walker

Publisher
John Wiley and Sons
Year
1969
Tongue
English
Weight
337 KB
Volume
58
Category
Article
ISSN
0022-3549

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✦ Synopsis

A series of 9-alkyl aromatic 8-carbolines was synthesized and evaluated as inhibitors of mitrochondrial monoamine oxidase.

The possible existence of a hydrophobic or hydrophilic region on the enzyme was explored. Substitution of an electron-withdrawing group such as acetyl on N-9 position reduced the inhibitory activity. This suggested that the increase in the inhibitory activity of 9- methyl-p-carboline was at least partially due to the increase of its electron density by the methyl group, thus making the p-carboline bind better to the enzyme.

Keyphrases 0 Monoamine oxidase (MAO) inhibitors-synthesis 0 8-Carbolines, 9-substituted-synthesis 0 Pharmacological screening-p-carbolines, M A 0 inhibitors IR spectrophotometrystructure 0 UV spectrophotometry-structure

📜 SIMILAR VOLUMES

Inhibitors of monoamine oxidase IV: 6(or
Inhibitors of monoamine oxidase IV: 6(or 8)substituted tetrahydro-β-carbolines and their 9-methyl analogs
✍ Beng T. Ho; William M. McIsaac; L. Wayne Tansey 📂 Article 📅 1969 🏛 John Wiley and Sons 🌐 English ⚖ 498 KB

Several analogs of tetrahydro-p-carboline (I) and 9-methyltetrahydro-p-carboline (VII) with substituents on C-6 or C-8 were synthesized. Methylation of the N-9 position of a tetrahydro p-carboline is generally achieved in the presence of a base. However, the preparations of 8,9-dimethyltetrahydro-p-