Potential antidepressant-like effect of piperazine derivative LQFM212 in mice: Role of monoaminergic pathway and brain-derived neurotrophic factor

Moreira, Lorrane Kelle da Silva; Brito, Adriane Ferreira de; Silva, Dayane Moreira da; Siqueira, Lorrayne; Silva, Daiany Priscilla Bueno da; Cardoso, Carina Sofia; Florentino, Iziara Ferreira; Carvalho, Pablinny Moreira Galdino de; Ghedini, Paulo César; Menegatti, Ricardo; Costa, Élson Alves

doi:10.1016/j.bbr.2020.113066

Cited by 4 publications

(2 citation statements)

References 51 publications

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“…Various excellent review articles have been published in the past few years describing the recent developments in the medicinal and biological perspectives of antidepressants agents [ 81 - 83 ]. Siddiqui et al and Singh et al reviewed the antidepressant potential of nitrogen-containing heterocyclic moieties [ 83 , 84 ], while the antidepressant perspective of piperazine derivatives has been compiled by Moreira et al [ 85 ]. Further, SAR and medicinal chemistry of indole-based antidepressant agents have been reviewed by Garg et al [ 86 ].…”

Section: Introductionmentioning

confidence: 99%

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents

Singh

Bhatia

Kumar

et al. 2022

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: Depression is one of the major disorders of the central nervous system worldwide and causes disability and functional impairment. According to the World Health Organization, around 265 million people worldwide are affected by depression. Currently marketed antidepressant drugs take weeks or even months to show anticipated clinical efficacy but remain ineffective in treating suicidal thoughts and cognitive impairment. Due to its multifactorial complexity, single-target drugs did not always produce satisfactory results and lacks the desired level of therapeutic efficacy. Recent literature reports revealed improved therapeutic potential of multi-target directed ligands due to their synergistic potency and better safety. Medicinal chemists have gone to great extents for the design of multi-target ligands by generating structural hybrids of different key pharmacophores with improved binding affinities and potency towards different receptors or enzymes. This article compiled the design strategies of recently published multi-target directed ligands as antidepressant agents. Their biological evaluation, structural-activity relationships, mechanistic and in silico studies were also described. This article will be highly useful for the researchers to design and develop multi-target ligands as antidepressants with high potency and therapeutic efficacy.

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Section: Introductionmentioning

confidence: 99%

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents

Singh

Bhatia

Kumar

et al. 2022

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“…Also, their antidepressant effects have been widely documented, for example, the marketed drugs Amooxapine, Sertraline, and Vilazodone (Figure 1) have piperazine fragments in their chemical structure. It has been reported that the introduction of piperazine fragments into appropriate compounds can also significantly improve the antidepressant activity of those compounds [9,10].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and In Vivo and In Silico Evaluation of Coumarin Derivatives with Potential Antidepressant Effects

et al. 2021

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In this study, a series of coumarin derivatives were designed and synthesized, their structures were characterized using nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS) testing methods. In the pharmacological experiment, two behavior-monitoring methods, the forced swim test (FST) and the tail suspension test (TST), were used to determine the antidepressant activity of coumarin derivatives. Compounds that showed potential activity were analyzed for their effects on 5-hydroxytryptamine (5-HT) levels in the brains of mice. Molecular docking experiments to simulate the possible interaction of these compounds with the 5-HT1A receptor was also be predicted. The results of the pharmacological experiments showed that most coumarin derivatives exhibited significant antidepressant activity. Among these compounds, 7-(2-(4-(4-fluorobenzyl)piperazin-1-yl)-2-oxoethoxy)-2H-chromen-2-one (6i) showed the highest antidepressant activity. The results of the measurement of 5-HT levels in the brains of mice indicate that the antidepressant activity of coumarin derivatives may be mediated by elevated 5-HT levels. The results of molecular docking demonstrated that compound 6i had a significant interaction with amino acids around the active site of the 5-HT1A receptor in the homology model. The physicochemical and pharmacokinetic properties of the target compounds were also predicted using Discovery Studio (DS) 2020 and Chemdraw 14.0.

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Anxiolytic- and antidepressant-like effects of new phenylpiperazine derivative LQFM005 and its hydroxylated metabolite in mice

Moreira

Silva

et al. 2022

Behavioural Brain Research

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Potential antidepressant-like effect of piperazine derivative LQFM212 in mice: Role of monoaminergic pathway and brain-derived neurotrophic factor

Cited by 4 publications

References 51 publications

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents

Design, Synthesis, and In Vivo and In Silico Evaluation of Coumarin Derivatives with Potential Antidepressant Effects

Anxiolytic- and antidepressant-like effects of new phenylpiperazine derivative LQFM005 and its hydroxylated metabolite in mice

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