An overview of structurally diversified anticonvulsant agents

Abstract

There are several limited approaches to treat epilepsy in hospitals, for example, using medicines, surgery, electrical stimulation and dietary interventions. Despite the availability of all these new and old approaches, seizure is particularly difficult to manage. The quest for new antiepileptic molecules with more specificity and less CNS toxicity continues for medicinal chemists until a new and ideal drug arrives. This review covers new antiseizure molecules of different chemical classes, the exact mode of action of which is still unidentified. Newer agents include sulfonamides, thiadiazoles, semi- and thiosemicarbazones, pyrrolidine-2,5-diones, imidazoles, benzothiazoles and amino acid deriva tives. These new chemical entities can be useful for the design and development of forthcoming antiseizure agents.

Design, synthesis and anticonvulsant activity of new Diacylthiosemicarbazides

“…Yield: 70 %; 5.15;N,14.32;S,10.93;Found: C,53.29;H,5.21;N,14.38;S,acetyl)hydrazine-1-carbonothioyl)cyclopropanecarboxamide (2.3) 4.89;N,13.58;S,20.72;Found: C,50.53;H,4.93;N,14.04;S,Benzoylhydrazine-1-carbonothioyl) cyclopropanecarboxamide (2.4). Yield: 75 %; 6 Hz,2H,6),3H,4,5) 5.07;N,20.13;S,11.52 ;Found: C,51.82;H,5.13;N,20.18;S,11.59. (2.6) ,4.58;N,21.20;S,12.13;Found: C,50.03;H,4.60;N,21.16;S,12.18.…”

“…Accessed September 6, 2020]. The choice of biological targets was due to the literature on the mechanism of antiepileptic drugs activity [1,5,21,22].…”

“…They cannot be considered perfect because of insufficient effectiveness and safety. They have significant side effects and cannot adequately control seizures in some cases [1][2][3][4][5]. However, the drugs of the last generation (valproate, vigabatrin, gabapentin, pregabalin, felbamate, tiagabine, topiramate etc.)…”

Thiazole-Bearing 4-Thiazolidinones as New Anticonvulsant Agents

“…One of the main achievements in the anticonvulsant thiazolidinones area is the ralitolin -(2Z)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-4-oxo-1,3thiazolidine-2-ylidene)-acetamide and phenytoin -5,5-diphenyl-2,4-imidazolidinedione, which are proved anticonvulsant drugs. Moreover, thiazolidinone derivatives correspond to the structural requirements to new anticonvulsant structure: i) Contain cyclic imide or N-CO-CN fragments [20]; ii) involve the combination of two aromatic rings as hydrophobic domain; iii) contain N=C-NH moiety as hydrogen bonding domain; iv) contain carbonyl group as the electron donor group [21][22][23][24][25][26] (Figure 1). Among different thiazolidinone subtypes, 5-substituted 2-amino(imino)-4-thiazolidinones [27] and 2-R-substituted-4-thiazolidinones are the most discussed compounds with confirmed anticonvulsant activity [28][29][30][31].…”

β-Naphthalene Incorporated Thiazole-5-Carboxamides/Thiazole -5- Ketones: Design, Synthesis and Anticonvulsant Screening against Two Seizure Models

“…Epileptic seizures are episodes that can differ from brief and nearly unnoticeable to long periods of forceful shaking. In the brain, epilepsy causes unusual release of neurotransmitters due to which the electrical working of brain gets disturbed prompting muscle spasm, nausea, convulsions and loss of consciousness (Al-Otaibi, 2019). It can be triggered by brain injuries, tumours, high fevers or strokes.…”