Design, Synthesis, and Pharmacological Evaluation of Novel 2‐(4‐substituted piperazin‐1‐yl)1, 8 Naphthyridine 3‐Carboxylic Acids as 5‐HT3 Receptor Antagonists for the Management of Depression

doi:10.1111/cbdd.12370

Paper

Design, Synthesis, and Pharmacological Evaluation of Novel 2‐(4‐substituted piperazin‐1‐yl)1, 8 Naphthyridine 3‐Carboxylic Acids as 5‐HT3 Receptor Antagonists for the Management of Depression

Published Dec 1, 2014 · A. Dhar, R. Mahesh, A. Jindal

Chemical Biology & Drug Design

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Abstract

1, 8‐naphthyridine‐3‐carboxylic acid analogs were synthesized and found to possess potential 5‐HT3 receptor antagonism as well as antidepressant‐like activity. Initially, 5‐HT3 receptor antagonism of all the compounds was determined in the form of pA2 value against agonist 2‐methyl 5‐HT in longitudinal muscle–myenteric plexus preparation from guinea‐pig ileum. Among all the compounds tested, compound 7a demonstrated most promising pA2 value of 7.6. Subsequently, all the compounds were evaluated for antidepressant activity using forced swim test and tail suspension test in mice. Compounds 7a, 7d, 7f, 7h, and 7i exhibited significant (p < 0.05) antidepressant‐like activity as compound to vehicle‐treated group. Importantly, none of the tested compound affected locomotor activity of mice at tested dose levels.

Non-RCT

Animal Study

Study Snapshot

Novel 1,8-naphthyridine-3-carboxylic acid analogs show potential as 5HT3 receptor antagonists and exhibit antidepressant-like activity without affecting locomotor activity in mice.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Design, Synthesis, and Pharmacological Evaluation of Novel 2‐(4‐substituted piperazin‐1‐yl)1, 8 Naphthyridine 3‐Carboxylic Acids as 5‐HT3 Receptor Antagonists for the Management of Depression

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The novel 3-ethoxyquinoxalin-2-carboxamides show promising anti-depressant-like activity, with compound 6h showing the most activity in guinea pig ileum preparations.

Design, synthesis and structure-activity relationship of novel quinoxalin-2-carboxamides as 5-HT3 receptor antagonists for the management of depression.

Novel quinoxalin-2-carboxamides show potential as 5-HT3 receptor antagonists for depression treatment, with some showing good anti-depressant-like activity without affecting mice locomotion.

Citations

Synthesis of 1, 8-Naphthyridine-3-Carbonitriles under solvent-free conditions using ceric ammonium nitrate

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Recent advances with 5-HT3 modulators for neuropsychiatric and gastrointestinal disorders.

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Compound 7e exhibits antidepressant-like effects and anxiolytic-like effects in behavioral rodent models of depression and anxiety.

1,8‐Naphthyridine Derivatives: A Review of Multiple Biological Activities

1,8-naphthyridine derivatives show diverse biological activities, including antimicrobial, antiviral, anticancer, anti-inflammatory, and analgesic properties, making them potential therapeutic and medicinal scaffolds.