scholarly journals Comparative studies on the anticonvulsant activity of lipophilic derivatives of .GAMMA.-aminobutyric acid and 2-pyrrolidinone in mice.

1991 ◽  
Vol 14 (1) ◽  
pp. 1-8 ◽  
Author(s):  
Junzo NAKAMURA ◽  
Takaichi MIWA ◽  
Yoshiyuki MORI ◽  
Hitoshi SASAKI ◽  
Juichiro SHIBASAKI
Keyword(s):  
Comparative Studies ◽  
Anticonvulsant Activity ◽  
Aminobutyric Acid ◽  
Gamma Aminobutyric Acid ◽  
Derivatives Of

Novel 3-Substituted-2, 3-Dihydro-2-Thioxoquinazolin-4-(1H)-one derivative as Anticonvulsants: Synthesis, Molecular Docking and Pharmacological Screening

2020 ◽  
Vol 17 (6) ◽  
pp. 757-771 ◽  
Author(s):  
Nimisha jain ◽  
Pradeep Kumar Singour
Keyword(s):  
Molecular Docking ◽  
Anticonvulsant Activity ◽  
Type A ◽  
Docking Study ◽  
Aminobutyric Acid ◽  
World Health ◽  
Maximal Electroshock ◽  
Gamma Aminobutyric Acid ◽  
Molecular Docking Study ◽  
Acid Type

Background: According to the World Health Organization, 50 million people worldwide are suffering from epilepsy, making it one of the most common neurological diseases globally. 2,3 disubstituted quinazolinone-4-one derivatives endowed with various pharmacological activity, particularly having anticonvulsant action. Objectives: The aim of this study was to synthesize 3-Substituted-2,3-Dihydro-2-thioxoquinazolin- 4-(1H)-one derivative and evaluate for anticonvulsant activity and neurotoxicity in order to find an efficient, compound with lesser side effects. Methods: A novel series of 3-[4-(2-amino-5, 6-dihydro-4(substituted phenyl)-4H-1, 3-oxazin /thiazin-6yl) phenyl]-2, 3-dihyro-2-thioxoquinazolin-4(1H)-one derivatives (4a-4p) were synthesized. The structures of the synthesized compounds were assigned on the basis of spectral data (UV, IR, 1HNMR, 13CNMR and MS) and performed anticonvulsant activity against maximal electroshock test and Subcutaneous Pentylenetetrazole model. Neurotoxicity was assessed using a rotarod apparatus test. The molecular docking study was performed to assess their binding affinities towards Gamma-Aminobutyric Acid type A receptor. A quantitative estimate of drug-likeness was also performed, which calculates the molecular properties and screen the molecules based on drug-likeness rules. Results: Compounds 4b, 4e, 4j and 4m have shown the highest anticonvulsant activity against tonic seizure with decreased mean duration of tonic hind leg extension of 8.31, 7.35, 8.61 and 8.99 s, respectively in maximal electroshock model and increased onset time clonic convulsion duration of 94.45, 96.65, 93.51 and 91.86 s in Subcutaneous Pentylenetetrazole model. Molecular docking study revealed a better binding affinity with Gamma-Aminobutyric Acid type A receptor. Conclusion: The compound 4b and 4e emerged out as the pilot molecule with a better anticonvulsant activity without any neurotoxicity. The obtained results showed that compounds 4b and 4e could be useful as a template for future design, optimization, and investigation to produce more active analogs.

scholarly journals ANTICONVULSANT PROPERTIES OF SOME MEDICINAL PLANTS- A REVIEW

2017 ◽  
Vol 10 (2) ◽  
pp. 109
Author(s):  
Nivedha Srinivasan ◽  
Anitha Roy
Keyword(s):  
Medicinal Plants ◽  
Anticonvulsant Activity ◽  
Persea Americana ◽  
Aminobutyric Acid ◽  
Anticonvulsant Effect ◽  
Gamma Aminobutyric Acid ◽  
Brain Disorder ◽  
Root Stock ◽  
The Brain ◽  
Boerhavia Diffusa

Introduction: Epilepsy is the tendency to have seizures that start in the brain. The brain uses electrical signals to pass messages between brain cells and when these signals are disrupted, it leads to a seizure. A number of synthetic antiepileptic drugs are available in practice, but various medicinal plants act as an important source of treatment for epilepsy; plants such as Aeollanthus suaveolens, Passiflora caerulea, Persea americana, Annona diversifolia, and Boerhavia diffusa have good anticonvulsant activity.Objective: Anticonvulsant drugs are used to control the convulsions by inhibiting the discharge and then producing hypnosis. The objective is to understand various medicinal plants and plant components, which are being used as an anticonvulsant.Results: A. suaveolens essential oils are the main constituents were deemed to display anticonvulsant activity. P. caerulea is reputed to have herbal activity as a sedative and anticonvulsant and it is often used as a relatively disease resistant root stock. Whereas P. americana, extract produces its anticonvulsant effect by enhancing gamma-aminobutyric acid ergic neurotransmission and or action in the brain. B. diffusa consists of a calcium channel antagonist compound, liriodendrin that is responsible for its anticonvulsant activity.Conclusion: Since epilepsy has become a common brain disorder, having knowledge of the medicinal plants with an anticonvulsant activity will be beneficial to the society.Keywords: Antiepileptic, Aeollanthus suaveolens, Passiflora caerulea, Persea americana, Annona diversifolia, Boerhavia diffusa.

НОВЫЕ ПОТЕНЦИАЛЬНЫЕ ПРОТИВОСУДОРОЖНЫЕ СРЕДСТВА В РЯДУ N-ПАРА-ЗАМЕЩЕННЫХ НЕЙРОАМИНОКИСЛОТ И ИХ ЛИТИЕВЫХ ПРОИЗВОДНЫХ / NEW POTENTIAL ANTICONVULSANT COMPOUNDS IN A NUMBER OF N-PARA-SUBSTITUTED NEUROAMINO ACIDS AND THEIR LITHIUM DERIVATIVES

2021 ◽  
pp. 82-88
Author(s):  
Ruzanna Paronikyan ◽  
Sedrak Ghazaryan ◽  
Iren Barkhudaryants ◽  
Gyulnara Matsakyan ◽  
Frederick Thomas Greenaway
Keyword(s):  
Anticonvulsant Activity ◽  
Aminobutyric Acid ◽  
Lithium Salts ◽  
Biological Value ◽  
Gaba Derivatives ◽  
Derivatives Of

Изучены степени противосудорожной активности некоторых N-пара-замещенных производных γ-аминомасляная кислоты и их литиевых солей. Все исследованные соединения проявляют противосудорожную активность по антагонизму с коразолом и тиосемикарбазидом. Новые синтезированные производные ГАМК представляют биологическую ценность как новые нейротропные вещества, обладающие противосудорожными свойствами. / The degrees of anticonvulsant activity of some N-para-substituted derivatives of γ-aminobutyric acid and their lithium salts were studied. All studied compounds exhibit anticonvulsant activity in antagonism with corazole and thiosemicarbazide. Newly synthesized GABA derivatives are of biological value as new neurotropic substances with anticonvulsant properties.

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