Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

doi:10.1016/j.bmcl.2010.09.081

Paper

Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

Published 2010 · Jong Yup Kim, Deukjoon Kim, S. Kang

Bioorganic & medicinal chemistry letters

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20

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0

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Abstract

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Study Snapshot

Pyrimidine derivatives targeting serotonin receptors and transporter show potential antidepressant activity in a forced swimming test animal model, with no appreciable inhibitory activity against hERG channel blocking assay.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

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References

Citations

Amphetamine Derivatives as Potent Central Nervous System Multitarget SERT/NET/H3 Agents: Synthesis and Biological Evaluation.

Compound 11b shows potential as a multifaceted antidepressant agent by inhibiting serotonin and noradrenaline transporters and histamine H3 receptor, with favorable pharmacokinetic profiles in rats.

Efficient synthetic strategies for fused pyrimidine and pyridine derivatives: A review

This review highlights the importance of various catalysts and ring substitution in synthesizing fused pyrimidine derivatives, which play a crucial role in drug discovery.

Novel Nanomolar Allosteric Modulators of AMPA Receptor of Bis(pyrimidine) Series: Synthesis, Biotesting and SAR Analysis

Novel bis(pyrimidines) show potential as potent AMPA receptor modulators, with 2-methyl-4-(4-((2-methyl-5,6,7,8-tetrahydroquinazolin-4-yl)oxy)phenoxy)-6,7,8,9-tetrahydro

Insights into the structure activity relationship of nitrogen-containing heterocyclics for the development of antidepressant compounds: An updated review

Nitrogen-based heterocyclics play a crucial role in the development of antidepressant compounds, with potential for improved potency and reduced toxicity through multiple mechanisms.

Synthesis, Anticonvulsant and Antinociceptive Activity of New Hybrid Compounds: Derivatives of 3-(3-Methylthiophen-2-yl)-pyrrolidine-2,5-dione

New hybrid compounds with pyrrolidine-2,5-dione and thiophene rings show potential as anticonvulsant and antinociceptive agents, with the most promising compound showing higher anticonvulsant activity than valproic acid and ethosuximide.

Computational Modeling and Pharmacokinetics/ADMET Study of Some Arylpiperazine Derivatives as Novel Antipsychotic Agents Targeting Depression

Arylpiperazine derivatives show potential as novel antidepressant agents with SpMax6_Bhm playing a predominant role and low ADMET risk, based on computational modeling and pharmacokinetic/ADMET properties.