Literature DB >> 32468477

Synthesis and Characterization of Biologically Significant 5-[N,N-dialkylamino alkoxy] azaindole 2-one, 3-thiosemicarbazones and 5-[N,N-dialkylamino alkoxy] azaindole 3-hydrazone, 2-ones.

Konda Swathi1, Galla Rajitha2, Manda Sarangapani3.   

Abstract

In the present work, new indole derivatives, i.e., 5-[N,N-di alkyl amino alkoxy] azaindole 2,3- di-one derivatives, are synthesized and characterized. These compounds were subjected to acute toxicity and then screened for antiepileptic activity on maximal electroshock seizure (MES) model in albino Wistar rats. In that study 5-[2-dimethyl amino ethoxy] Azaindole-3-hydrazone,2-one and 5-[2- dimethyl amino ethoxy] Azaindole 2-one,3-thiothiosemicarbazone(IIIa) showed good antiepileptic activity and less neurotoxicity compared to phenytoin. The purpose of the present study is to investigate the effect of 5-[2-dimethyl amino ethoxy] Indole 2,3- di one and 5-[2-dimethyl amino ethoxy] Azaindole 2-one,3-thiosemicarbazone(IIIa) derivatives on biogenic amines concentrations in rat brain after induction of seizures by MES method. The aim of study was relationship between seizure activities and altered the monoamines such as Noradrenaline (NA), Dopamine (DA), Serotonin (5-HT) in forebrain of rats in MES seizure models. In MES model, study of 5-[2-dimethyl amino ethoxy] Azaindole 3-hydrazone,2-one(Va) and 5-[2-dimethyl amino ethoxy]Azaindole 2-one,3-thiosemicarbazone(IIIa) (100 mg/kg) showed significant restoration of the decreased levels of brain monoamines such as noradrenaline, dopamine, and 5-hydroxytryptamine. Thus, this study suggests that 5-[2-Dimethyl amino ethoxy] Azaindole 3-hydrazone,2-one (V) and 5-[2-dimethyl amino ethoxy] Azaindole 2-one,3-thiosemicarbazone (IIIa) increased the monoamines on rat brain, which may decrease the susceptibility to MES-induced seizure in rats.

Entities:  

Keywords:  5-HT; 5-[N,N-dialky amino alkoxy] Azaindole 2-ones, 3-thiosemicarbazones; 5-[N,N-dialky amino alkoxy] Azaindole 3-hydrazones, 2-ones; Antiepileptic activity; Biogenic amines; DA; NA

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Year:  2020        PMID: 32468477     DOI: 10.1007/978-3-030-32633-3_27

Source DB:  PubMed          Journal:  Adv Exp Med Biol        ISSN: 0065-2598            Impact factor:   2.622


  7 in total

1.  Kindling-based status epilepticus: effect of norepinephrine depletion with 6-hydroxydopamine.

Authors:  D C McIntyre; N Edson
Journal:  Exp Neurol       Date:  1989-04       Impact factor: 5.330

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Authors:  C D Applegate; J L Burchfiel; R J Konkol
Journal:  Exp Neurol       Date:  1986-11       Impact factor: 5.330

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Authors:  S N Pandeya; P Yogeeswari; J P Stables
Journal:  Eur J Med Chem       Date:  2000-10       Impact factor: 6.514

4.  Neurochemical effects of electrically and chemically induced seizures: an in vivo microdialysis study in the rat hippocampus.

Authors:  A P Zis; G G Nomikos; E E Brown; G Damsma; H C Fibiger
Journal:  Neuropsychopharmacology       Date:  1992-11       Impact factor: 7.853

5.  Characteristics of accelerated kindling after depletion of noradrenaline in adult rats.

Authors:  M E Corcoran
Journal:  Neuropharmacology       Date:  1988-10       Impact factor: 5.250

6.  Infusions of alpha-2 noradrenergic agonists and antagonists into the amygdala: effects on kindling.

Authors:  M R Pelletier; M E Corcoran
Journal:  Brain Res       Date:  1993-12-31       Impact factor: 3.252

  7 in total

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