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Relevant academic research and scientific papers

6-Hydroxy- and 6-methoxy-β-carbolines as acetyl- and butyrylcholinesterase inhibitors

In the course of studies directed toward the discovery of novel acetyl- and butyrylcholinesterase (AChE and BChE) inhibitors for the treatment of Alzheimer's disease, we focused on β-carbolines (BCs). 6-Oxygenated β-carboline and β-carbolinium derivatives based on the serotonin template were synthesized and tested in vitro for their ability to inhibit AChE and BChE, respectively. Particularly the carbolinium salts, which can be formed by intracerebral methylation out of the tertiary-BC prodrugs, show inhibitory activity levels reaching those of galantamine, physostigmine, and rivastigmine.

Substituted beta-carbolines

Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of IκB kinase is involved.

Carbolines. Part VII. Anisidines, convenient tools to synthesize hydroxy-β-carbolines

The paper describes a convenient synthesis of hydroxy-β-carbolines from commercial anisidines based on key steps such as metalation, cross-coupling and cyclization. The first total synthesis of a major cytotoxic constituent of a marine bryozoan is also re

A convenient synthesis of 6-hydroxyharman

A three-step synthesis of 6-hydroxyharman and 6-hydroxynorharman from benzene and pyridine blocks is described. The preparation of the two α-substituted β-carbolines is based on a new synthetic methodology which involves reactions such as Directed Ortho M

Indoles, XII: β-Carbolines from lactones - Synthesis of ligands of the norharmane receptor

Starting from α-ethoxalyl-δ-valerolactone (1) 6-substituted β-carbolines were synthesized in 5 steps to enable investigations at the norharmane binding sites in rat liver and in pig brain. The Pd-catalyzed aromatization of N-benzyl-tetrahydro-β-carbolines with debenzylation was optimized with 5a → 6a and then used for the preparation of other derivatives. Additional hydrogenolyses occur with 5d,h. Bromination of 1a gives 6d which can be transferred to the radioligand 3H-norharmane.

Eudistomin derivatives, novel phosphodiesterase inhibitors: Synthesis and relative activity

The preparations of novel phosphodiesterase inhibitors, 8-acetoxy-5-iodo-6-methoxypyrido[3,4-b]indole, 5,7-dibromo-6-hydroxypyrido[3,4-b]indole, 5,7-dichloro-6-hydroxypyridol[3,4-b]indole and 8-acetoxy-5-bromo-6-methoxypyrido[3,4-b]indole, are described together with concentrations giving 50% inhibition against cycle AMP phosphodiesterase, i.e. 3 x 10-6, 3 x 10-, 7 x 10-6 and 1 x 10-5 M, respectively. The relative potency of these eudistomin derivatives is discussed in terms of the chemical structures compared with those of other inactive eudistomins and derivatives.