scholarly journals Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects

Marine Drugs ◽  
2019 ◽  
Vol 17 (7) ◽  
pp. 430 ◽  
Author(s):  
Qinghao Jin ◽  
Zhiyang Fu ◽  
Liping Guan ◽  
Haiying Jiang

Thirty-four new benzo[d]thiazol derivatives 2a–2i, 3a–3r, and 4a–4g were synthesized and investigated for their potential antidepressant and anticonvulsant effects. In a forced swimming test, 2c and 2d showed the highest antidepressant and anticonvulsant effects. 2c and 2d displayed a higher percentage decrease in immobility duration (89.96% and 89.62%, respectively) than that of fluoxetine (83.62%). In the maximal electroshock seizure test, 3n and 3q showed the highest anticonvulsant effect, with ED50 values of 46.1 and 64.3 mg kg−1, and protective indices of 6.34 and 4.11, respectively, which were similar to those of phenobarbital or valproate. We also found that the mechanism for the antidepressant activity of 2c and 2d may be via increasing the concentrations of serotonin and norepinephrine.

Author(s):  
Ajoy Borah ◽  
Binita Singha ◽  
Swopna Phukan

Objective: Depression is a major psychiatric disorder affecting nearly 350 million people worldwide and imposes a substantial health burden on the society. Ceftriaxone has demonstrated neuroprotective effects in animals. It has also undergone trials as a treatment option for amyotrophic lateral sclerosis. This study was therefore undertaken to evaluate the antidepressant-like effect of ceftriaxone in mice.Methods: Ceftriaxone was administered at three different doses (0.130, 0.195 and 0.260g/kg) to Swiss albino mice of either sex by intra peritoneal (i. p.) route. The period of immobility in control and drug-treated mice were recorded in forced swimming test (FST) and tail suspension test (TST). The antidepressant effect of ceftriaxone indicated by the decrease in duration of immobility was compared to that of fluoxetine (0.020 g/kg, i. p.).Results: Ceftriaxone decreased the duration of immobility in mice. It showed a significant dose-dependent antidepressant effect. The antidepressant effect of 0.260g/kg of ceftriaxone was comparable to that of fluoxetine in the TST but not in the FST.Conclusion: The results of the present study indicate antidepressant activity of Ceftriaxone. The study shows that ceftriaxone has additional action on the central nervous system other than neuroprotection. Ceftriaxone therapy in cases of encephalomeningitis and in various cases of hemorrhages in the brain can, therefore, prevent the development of depression in future


2012 ◽  
Vol 2012 ◽  
pp. 1-12 ◽  
Author(s):  
Lieh-Ching Hsu ◽  
Yu-Jen Ko ◽  
Hao-Yuan Cheng ◽  
Ching-Wen Chang ◽  
Yu-Chin Lin ◽  
...  

This study investigated the antidepressant activity of ethanolic extract ofU. lanosaWallich var.appendiculataRidsd (ULEtOH) for two-weeks administrations by using FST and TST on mice. In order to understand the probable mechanism of antidepressant-like activity of ULEtOHin FST and TST, the researchers measured the levels of monoamines and monoamine oxidase activities in mice brain, and combined the antidepressant drugs (fluoxetine, imipramine, maprotiline, clorgyline, bupropion and ketanserin). Lastly, the researchers analyzed the content of RHY in the ULEtOH. The results showed that ULEtOHexhibited antidepressant-like activity in FST and TST in mice. ULEtOHincreased the levels of 5-HT and 5-HIAA in cortex, striatum, hippocampus, and hypothalamus, the levels of NE and MHPG in cortex and hippocampus, the level of NE in striatum, and the level of DOPAC in striatum. Two-week injection of IMI, CLO, FLU and KET enhanced the antidepressant-like activity of ULEtOH. ULEtOHinhibited the activity of MAO-A. The amount of RHY in ULEtOHwas 17.12 mg/g extract. Our findings support the view that ULEtOHexerts antidepressant-like activity. The antidepressant-like mechanism of ULEtOHmay be related to the increase in monoamines levels in the hippocampus, cortex, striatum, and hypothalamus of mice.


Author(s):  
Tanmoy Gangopadhyay ◽  
Ananya Mandal ◽  
Uma Shanker Keshri

Background: Individuals with epilepsy have a higher incidence of psychiatric disorders than person without epilepsy. Epidemiological studies have shown that the co-morbidity of epilepsy and depression to be high as 50%. The conventional anti-depressants are believed to lower the seizure threshold making it difficult to treat the co-morbid depression, but animal studies have shown SSRIs, a common anti-depressant, to have anti-convulsant properties. So, we propose to study the anticonvulsant effects of fluoxetine, a SSRI, in albino rats against maximal electroshock seizure and to compare against a standard antiepileptic drug phenytoin.Methods: The anticonvulsant effect of fluoxetine was observed in model of maximal electroconvulsive seizure threshold in albino rats. The animals were divided into 3 groups having 6 animals each, receiving distilled water, fluoxetine and phenytoin respectively. The drugs were given orally, and the effect was observed on day 7, 14 and 21. Tonic hind-limb extension was taken as the parameter of electroshock seizure. The effects were compared against a standard anti-seizure drug phenytoin.Results: Fluoxetine showed significant elevation of the seizure threshold following 14 days of administration (P value 0.031). The effect was comparable to phenytoin with no significant difference after 7, 14 and 21 days of treatment (P-value 0.485, 0.699 and 0.818 respectively) though phenytoin showed significant anti-seizure effect since day 7 of treatment.Conclusions: Fluoxetine showed significant anti-seizure activity against electroconvulsive seizure in albino rats.


Author(s):  
Hansraj Kumar ◽  
Akash Chandra ◽  
Uma Shankar Prasad Keshri ◽  
Rajiv Kumar

Background: Depression is a group of disorders results from a combination of multiple etiologic factors- genetic, biochemical, psychodynamic and socio-environmental. A depression consists of following clinical features as sadness, apathy, changes in sleep pattern, impaired concentration, feeling of shame or guilt and thoughts of dying or death. Fluoxetine and riluzole both are used for the treatment of depression in human being. Fluoxetine is SSRI (selective serotonin reuptake inhibitors) and riluzole is anxiolytic and mood stabilizer.Methods: Healthy male albino rats weighing between 150-200 grams were taken for the present study. Study animals were divided into three groups randomly with each group consisting of ten animals. Drugs were powdered with help of mortar and pestle and mixed in gum acacia solution. Appropriate volume of the freshly prepared solution was administered orally daily between 9 am to 10 am to all animal as per their individual body weight. Group A administered 1ml of 0.9% normal saline orally and serves as control group. Group B administered 0.4 mg of fluoxetine orally. Group C administered 2 mg of riluzole orally. Animals were evaluated for antidepressant activity using model- forced swimming test.Results: The results in the forced swimming test were assessed by duration of immobility in last 4 minutes of total 6 minute test duration. Antidepressant activity is indicated by the reduction in the duration of immobility i.e. lesser the duration more the efficacy. The results have been expressed as mean±standard deviation of duration of immobility in seconds during 6 minute period.Conclusions: There was significant difference in antidepressant activity of fluoxetine with antidepressant activity of riluzole. Riluzole showed antidepressant activity after two weeks of starting the drugs.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 383
Author(s):  
Jovelina Samara Ferreira Alves ◽  
Alaine Maria dos Santos Silva ◽  
Rodrigo Moreira da Silva ◽  
Pamella Rebeca Fernandes Tiago ◽  
Thais Gomes de Carvalho ◽  
...  

A variety of neuroactive flavonoids can be found in the species of the Passiflora genus; however, their difficulty in crossing the blood–brain barrier limits their in vivo neuropharmacological activity. In this study, cationic nanoparticles were developed as a novel nanocarrier for improving the antidepressant activity of Passiflora edulis f. flavicarpa leaf extract. Formulations obtained using Eudragit E PO polymethylmethacrylate copolymer, as polymeric matrix had their physicochemical properties investigated. The analytical content of the flavonoids vicenin-2, orientin, isoorientin, vitexin, and isovitexin was determined in the plant extract. Small-sized and spherical nanoparticles loaded with Passiflora edulis f. flavicarpa were obtained with positive zeta potential and high encapsulation efficiency. In addition, the nanosystems were shown to be stable for at least 6 months. The antidepressant activity of P. edulis extract (50 and 100 mg/kg) as well as the extract-loaded nanoparticles (5 mg/kg) were investigated in mice using the forced swimming test, where the latter increased the potency of the former by 10-fold. In addition, histopathological and biochemical analysis confirmed the biocompatibility of the extract-loaded nanoparticles. This study demonstrated that the Eudragit cationic nanoparticles were able to improve the antidepressant activity of P. edulis in the central nervous system of mice.


2019 ◽  
Vol 15 ◽  
Author(s):  
Divya Chauhan ◽  
Syed Riaz Hashim ◽  
Priyanka Rani ◽  
Sushil Kumar ◽  
Navratan Shrimal ◽  
...  

Background : Privileged 4H-chromenes possess the potent anticancer and anticonvulsant actives. By inspiring potency of 4H-chromenes and demands of present era of scaffold, discovery of effective molecule was carried out for the treatment of cancer and conversant. Objective : Designed and synthesized a novel series of 4H-chromene derivatives from one port synthesis for the treatment of cancer and conversant. Method : Substitution of side amide chain was formed in multiple steps on amine group of chromene. Later, anticancer activity of synthesized compounds was investigated against human colon adenocarcinoma cell line (HT-29) using sulforhodamine B (SRB) assay. Moreover, anticonvulsant activity was also screened out by using maximal electroshock seizure (MES) model and subcutaneous Metrazol Seizure Threshold Test (scMET) in albino Wistar rats. Neurotoxicity was evaluated using by rotarod test. Before the synthesis, docking studies were performed using various molecular targets. Subsequently, the computational study of the titled compounds was performed to predict the pharmacokinetic profile. Result: Among the fifteen tested compounds, A4 and A9 were found to be active against HT-29 cells (growth inhibitory dose 50% (GI50) <11µM). Moreover, compounds A4 showed the protection at 300mg/kg in scMET (h) for albino Wistar rats and compounds A9, A11, A15 exhibited the anticonvulsant effect at the doses 100, 300 and 300 mg/kg, respectively in MES screen(h). Conclusion : Due to these encouraging results, we concluded that both A4 and A9 may be effective against colon cancer. While compound A9 may be used as a considerable effective molecule for the treatment of epilepsy.


Author(s):  
Salman Kapadia ◽  
Vanita Kanase

Background: Cissus quadrangularis has been used for cure of various ailments that includes bone cracks, frail bones (osteoporosis), scurvy, malignant growth, annoyed stomach, hemorrhoids, peptic ulcer sickness, excruciating menstrual periods, asthma, jungle fever (malaria), and mental distress. Specially it is used for bone healing properties. According to this background, the aim of the study was to evaluate the antidepressant-like effect of the ethanolic extract of Cissus quadrangularis (EECQ) in different behavioral models such as forced swimming test (FST) and tail suspension test (TST) on mice after two weeks treatment. Methods: Mice were divided into six groups (n=6/group): control group (normal saline), stress control (normal saline), standard group where Imipramine (15mg/kg) was used as standard drug and three test groups where three doses of ethanolic extract of C. quadrangularis (EECQ) (100, 250, and 350mg/kg) was used for two weeks treatment. All the medication and test samples were managed by means of gavage through oral course. To evaluate the antidepressant like impact of EECQ forced swim test (FST) and tail suspension test (TST) have been done in mice. Results: The outcomes demonstrated that a solid and dose-dependent antidepressant effects in various mice models. The main findings of the EECQ significantly decreased the duration of immobility times in the forced swimming test (p<0.5). Likewise, the extract significantly decreased the immobility time in the tail suspension test (p<0.5) when compared against stress control as well as against imipramine which was used as a standard. Conclusion: The present results clearly demonstrate that the ethanolic extract of C. quadrangularis possesses antidepressant-like activity in the animal behavioral models. Cissus quadrangularis plant can be used for the treatment of neurological disorders and may be recommended as a supplement for the antidepressant activity.


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