scholarly journals Thiazole-Bearing 4-Thiazolidinones as New Anticonvulsant Agents

2020 ◽  
Vol 88 (1) ◽  
pp. 16 ◽  
Author(s):  
Mariia Mishchenko ◽  
Sergiy Shtrygol ◽  
Danylo Kaminskyy ◽  
Roman Lesyk
Keyword(s):  
Acetic Acid ◽  
Carboxylic Acid ◽  
Anticonvulsant Activity ◽  
Acid Ethyl Ester ◽  
Alkylation Reaction ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
One Pot ◽  
Structural Requirements ◽  
Three Component Reaction

Here, we describe the synthesis and anticonvulsant activity of thiazole-bearing hybrids based on 2-imino-4-thiazolidinone and 2,4-dioxothiazolidine-5-carboxylic acid cores. The structure of target compounds was based on the following: (i) A combination of two thiazole cores; (ii) similarity to ralitolin’s structure; (iii) the compliance with structural requirements for the new anticonvulsants. Target compounds were synthesized via known approaches based on Knoenavegel reaction, alkylation reaction, and one-pot three-component reaction. Anticonvulsant properties of compounds were evaluated in two different models—pentylenetetrazole-induced seizures and maximal electroshock seizure tests. Among the tested compounds 5Z-(3-nitrobenzylidene)-2-(thiazol-2-ylimino)-thiazolidin-4-one Ib, 2-[2,4-dioxo-5-(thiazol-2- ylcarbamoylmethyl)-thiazolidin-3-yl]-N-(2-trifluoromethylphenyl)acetamide IId and (2,4-dioxo-5- (thiazol-2-ylcarbamoylmethylene)-thiazolidin-3-yl)acetic acid ethyl ester IIj showed excellent anticonvulsant activity in both models. The directions of compounds modification based on SAR aspects were discussed. The results of the study provide a basis for further study of the anticonvulsant properties of selected thiazole-thiazolidinones.

Evaluation of the Anticonvulsant Activity of Terpinen-4-ol

2009 ◽  
Vol 64 (1-2) ◽  
pp. 1-5 ◽  
Author(s):  
Damião P. de Sousa ◽  
Franklin F. F. Nóbrega ◽  
Liana C. S. L. de Morais ◽  
Reinaldo N. de Almeida
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Animal Models ◽  
Motor Activity ◽  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Aromatic Plants ◽  
Depressant Effect ◽  
Maximal Electroshock Seizure ◽  
The Central Nervous System

Terpinen-4-ol is a monoterpenoid alcohol and component of the essential oils of several aromatic plants. Similarly to terpinen-4-ol, other monoterpenoid alcohols have shown anticonvulsant activity in convulsion animal models. The present study aimed to investigate the anticonvulsant activity of terpinen-4-ol. Treatment of mice with terpinen-4-ol ( 200 mg/kg) caused a signifi cant decrease in the spontaneous motor activity at 30, 60 and 120 min after administration. Terpinen-4-ol (100 and 200 mg/kg) produced a significant dosedependent increase in the duration of sleeping in mice. Pretreatment of mice with terpinen-4- ol at doses of 100, 200 and 300 mg/kg significantly increased the latency of pentylenetetrazole -induced convulsions. Terpinen-4-ol (200 and 300 mg/kg) also inhibited the induced seizures of picrotoxin. In another model, maximal electroshock seizure, terpinen-4-ol decreased the tonic hind convulsions percentage at the dose of 300 mg/kg. From the overall results we can conclude that terpinen-4-ol showed a depressant effect on the central nervous system and significant anticonvulsant activity.

scholarly journals Synthesis One Pot of Alkyne-2-Chloroquinoline via a Passerini Reaction

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 76
Author(s):  
Sandra C. Ramírez-López ◽  
Rocío Gámez-Montaño
Keyword(s):  
Carboxylic Acid ◽  
Small Molecules ◽  
Passerini Reaction ◽  
One Pot ◽  
Protein Targets ◽  
Three Component Reaction ◽  
Green Conditions ◽  
In Cells

A series of six new alkyne-2-chloroquinolines were synthesized in moderate yields (40%–65%) via the Passerini three-component reaction (P-3CR) under mild green conditions. The P-3CR takes place when a carboxylic acid, an oxo compound (aldehyde or ketone), and an isocyanide react to give α-acyloxy carboxamides. Recently it has been reported that small molecules containing alkynes promote interactions with different proteins in cells facilitating the detection or identification of protein targets.

One-Pot Synthesis of Functionalised 4-Spiro-1,4-Dihydropyridines Via [1+2+1+2]-Cyclisation

2017 ◽  
Vol 41 (9) ◽  
pp. 513-516 ◽  
Author(s):  
Pan Zhou ◽  
Biao Hu ◽  
Lingling Lu ◽  
Rong Huang ◽  
Fuchao Yu
Keyword(s):  
Acetic Acid ◽  
Ammonium Acetate ◽  
Water Solution ◽  
Reaction Conditions ◽  
One Pot ◽  
Efficient Approach ◽  
H Nmr ◽  
Three Component Reaction ◽  
C Nmr ◽  
Operational Simplicity

A simple and efficient approach for the synthesis of 4-spiro-1,4-DHP derivatives has been developed, involving one-pot three-component reaction of isatins, N,N-dimethylenaminones with ammonium acetate in EtOH–water solution promoted by acetic acid. Compared with the previous [1+2+3]-cyclisation method, this [1+2+1+2]-cyclisation procedure has advantages as it is more environmentally friendly, has easier operational simplicity, and requires milder reaction conditions. Moreover, these novel compounds have been obtained in moderate to good yields and their structures have been confirmed by 1H NMR, 13C NMR and IR and HRMS spectroscopy.

Captopril potentiates the anticonvulsant activity of carbamazepine and lamotrigine in the mouse maximal electroshock seizure model

2010 ◽  
Vol 117 (10) ◽  
pp. 1161-1166 ◽  
Author(s):  
Krzysztof Łukawski ◽  
Tomasz Jakubus ◽  
Grzegorz Raszewski ◽  
Stanisław J. Czuczwar
Keyword(s):  
Anticonvulsant Activity ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Seizure Model

scholarly journals Synthesis of functionalized bicyclic pyridones containing dithiocarbamate group using thioazlactones, diamines and nitroketene dithioacetal

SynOpen ◽  
2021 ◽  
Author(s):  
Marziyeh Saeedi ◽  
maryam khoshdoun ◽  
Salman Taheri ◽  
Azim Ziyaei Halimehjani ◽  
Aliasghar Mohammadi ◽  
...  
Keyword(s):  
Alkylation Reaction ◽  
X Ray Diffraction ◽  
One Pot ◽  
Three Component Reaction ◽  
Reaction Proceeds ◽  
Ketene Dithioacetal ◽  
Ft Ir ◽  
High Yields ◽  
Nitro Ketene Dithioacetal ◽  
Dithiocarbamate Group

An efficient method for the synthesis of highly substituted bicyclic pyridone derivatives containing dithiocarbamate group is reported via a one-pot three-component reaction of 2-(alkylthio) thioazlactones, diamines and nitro ketene dithioacetal in EtOH under catalyst-free conditions. The reaction proceeds via a domino amidation/intramolecular 1,4-addition-type Friedel-Crafts alkylation reaction to afford the corresponding fused bicyclic pyridones with high yields and diastereselectively. The desired products are fully characterized by FT-IR, 1H and 13CNMR, CHN and single crystal X-ray diffraction analyses.

scholarly journals STUDY OF THE ANTICONVULSANT ACTIVITY OF ETHANOLIC EXTRACT OF ROOT OF ACORUS CALAMUS IN ALBINO RATS

2019 ◽  
Vol 12 (1) ◽  
pp. 185
Author(s):  
Shipra Kaushik ◽  
Kalpana Gohain
Keyword(s):  
Normal Saline ◽  
Anticonvulsant Activity ◽  
Ethanolic Extract ◽  
Albino Rats ◽  
Acorus Calamus ◽  
Maximal Electroshock ◽  
Maximal Electroshock Seizure ◽  
Onset Of Action ◽  
Electrical Shock ◽  
Seizure Models

Objective: Root of Acorus calamus has been traditionally used as an anticonvulsant. The aim of the study is to assess the anticonvulsant activity of ethanolic extract of A. calamus (EEAC) by maximal electroshock seizure (MES) and pentylenetetrazol (PTZ)-induced seizure models on albino (Wistar strain) rats.Methods: Albino rats were taken and divided into five groups, each consisting of five rats both for MES and PTZ model. One group was used as control (normal saline 10 ml/kg), one as standard (phenytoin in MES model/diazepam in PTZ model), and three groups for the test drug (EEAC in the doses of 100, 200, and 400 mg/kg). In MES model, maximal electrical shock of 150 mA was passed for 0.2 s through earlobe electrodes after 30 min of giving the drugs and normal saline. Different stages of convulsions were noted down along with time spent by the animal in each phase of convulsions. In PTZ model, PTZ was injected 30 min after giving the drugs and normal saline, and onset of action and severity of convulsions were noted. Data were statistically analyzed by one-way analysis of variance followed by multiple Dunnett’s test.Results: EEAC dose dependently reduced the duration of tonic hind limb extension in MES model, and there was increase in latency and occurrence of convulsions in PTZ model.Conclusion: EEAC has anticonvulsant activity.

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