Synthesis and Pharmacological Evaluation of Arylpiperazinyl Mannich Bases of 1‐(4‐Fluorobenzoyl)‐3‐acetyl Indole as 5‐Hydroxytryptamine and Dopamine Receptor Modulators in Mice

doi:10.1111/J.2042-7158.1998.TB00671.X

Paper

Synthesis and Pharmacological Evaluation of Arylpiperazinyl Mannich Bases of 1‐(4‐Fluorobenzoyl)‐3‐acetyl Indole as 5‐Hydroxytryptamine and Dopamine Receptor Modulators in Mice

Published Nov 1, 1998 · P. Srinivas, A. Subramanian, S. Raghavan

Pharmacy and Pharmacology Communications

UNKNOWN SJR score

1

Citations

0

Influential Citations

Full textSemantic Scholar

Abstract

We report the first synthesis of 1-(4-fluorobenzoyl)-3-acetyl indole (3) and its arylpiperazinyl mannich bases with potential 5-hydroxytryptamine and dopamine receptor modulatory activity. Treatment of 3-acetyl indole with 4-fluorobenzoyl chloride in the presence of anhydrous triethylamine in benzene gave 3 in good yields. Mannich reaction of 3 with substituted arylpiperazines and paraformaldehyde in ethanol gave the respective arylpiperazinyl mannich bases. Title compounds were tested for modulation of serotonergic (5-HT2) and dopaminergic (D1/D2) receptors in mice. The compounds showed moderate to good antagonism of D1/D2 receptors. A 4-methoxyphenyl piperazinyl mannich base of 3 showed good antagonism of the 5-HT2 receptor, and had a profile of an atypical antipsychotic.

Non-RCT

Animal Study

Study Snapshot

Arylpiperazinyl mannich bases of 1-(4-fluorobenzoyl)-3-acetyl indole show potential as 5-hydroxytryptamine and dopamine receptor modulators in mice, with a 4-methoxyphenyl piperazinyl mannich

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Paper

Synthesis and Pharmacological Evaluation of Arylpiperazinyl Mannich Bases of 1‐(4‐Fluorobenzoyl)‐3‐acetyl Indole as 5‐Hydroxytryptamine and Dopamine Receptor Modulators in Mice

Sign up to use Study Snapshot

References

Citations

3-Acetylindoles: Synthesis, Reactions and Biological Activities

3-acetylindoles have a wide range of biological activities, making them valuable compounds for treating various disorders and their synthesis and reactions are reviewed in this review.