Pharmacological Activity of Pyrazole Derivatives as an Anticonvulsant for Benefit against Epilepsy

Abstract

<b><i>Introduction:</i></b> Pediatric patients with epilepsy are prone to cognitive impairments during growth and long-term use of most antiepileptic drugs (AED). The affected children do not respond to conventional AED and may require novel drugs to manage the disease. Valproic acid, a first-line drug to treat epilepsy, is associated with serious side effects, which precludes its wider use. Thus, in the present study, we intended to develop novel substituted pyrazoles. <b><i>Methods:</i></b> The molecules were tested for anticonvulsive activity in Swiss albino mice via maximal electroshock seizure and subcutaneous pentylenetetrazole assays. The most potent molecule among the class was further assayed for its effect on behavioral and CNS depressant activity. The effect of the most potent compounds was also analyzed on various indices of oxidative stress and inflammation in mice. <b><i>Results:</i></b> The designed compounds showed significant anticonvulsive activity in mice revealing 7h as the most potent anticonvulsive agent. The most potent anticonvulsant molecule 7h further showed no behavioral alteration and considerable CNS depressant activity. It also reduces the level of oxidative stress and inflammation in the mice. <b><i>Conclusion:</i></b> Our study demonstrated utility of pyrazole derivatives as anticonvulsants against epilepsy.

“Microwave-Assisted, Solvent Free, One Pot Synthesis of Novel Bioactive Imidazolyl - Pyrazole derivatives catalyzed by Mesolite type Natural Zeolite”

“…Pyrazole and imidazole are five membered rings containing heterocyclic compound with two nitrogen's at 1, 2 and 1, 3 positions respectively. Pyrazole is five membered 1, 2-diazole heterocyclic compound and its moiety has number of biological activities such as antibacterial [1], antifungal [1,3], bacteriostatic [4], antibiofilm [5], Antioxidant [2,5], Anti-inflammatory activity [6], Anti-cancer [7], Anti-diabetic activity [8], insecticidal [9], Anti-convulsant activity [10], Anti-allergic activity, Herbicidal activity [11], antiviral [12], Antimalarial activity [13].…”

Recent Developments in the Synthesis of Indole‐Pyrazole Hybrids

“…Compound 6 on base-mediated hydrolysis followed by coupling with various amines resulted the target compounds (8 a-g). Similarly, 5-phenylpyrazolyl indoles (14 a-g) and 5benzylpyrazolyl indoles (22 b,d-h) were prepared starting from Further, the authors synthesized 4-phenylpyrazolyl indoles (27 a-c) and 5-benzylpyrazolyl indoles (31 a-e) by changing the substitutions at C3 position of indole (Scheme 2 & 3). Removal of Boc group from the compound 6 followed by Vilsmeier-Haack reaction led to the formation of 4-phenylpyrazolyl indole aldehyde (24) in good yield.…”

“…Research studies towards the synthesis of pyrazole‐containing heterocycles are growing rapidly due to their diverse pharmacological properties [16,17] . Several synthetic and naturally occurring pyrazole derivatives have been reported as potent anticancer, [18] antibacterial, antitumor, anti‐inflammatory, [19] antiviral, [20] antitubercular, [21] anticonvulsant, [22] antidepressant, analgesic and antipyretic agents [16,17] . Some of them were documented as potential epidermal growth factor receptor (EGFR) inhibitors, [23] vascular endothelial growth factor receptor (VEGFR‐2) inhibitors, [24] B‐Raf kinase inhibitors, [25] HIV‐1 RNase H inhibitors, [26] angiotensin converting enzyme (ACE) inhibitors, [27] estrogen receptor (ER) agonists [28] and cholecystokinin‐1 receptor antagonists [29] .…”

Synthesis and Evaluation of the Antiproliferative Potency and Induced Biochemical Parameters of Novel Pyrazolones Derivatives Towards Hepatocellular Carcinoma

“…The chemistry of pyrazolones and related compounds is particularly interesting because of their potential application in medicinal chemistry, as they have constituents of several intermediates for medicinal drugs [1]. Compounds with a pyrazoline structure have been found to possess anti-fungal [2], anti-depressant [3], anticonvulsant [4], anti-inflammatory [5],antibacterial [6][7], antipyretic [8] and antitumor [9][10] properties. Cancer is one of the most widespread serious diseases.…”