Prediction and Study of Anticonvulsant Properties of Benzimidazole Derivatives

Vasil’ev, P. M.; Kalitin, K. Yu.; Spasov, A. A.; Grechko, O. Yu.; Poroikov, Vladimir; Филимонов, Д. А.; Анисимова, В. А.

doi:10.1007/s11094-017-1530-6

Cited by 20 publications

(14 citation statements)

References 11 publications

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“…. Moreover, several benzimidazole derivatives are also shown to have seizure protective effects . Based on these observations and in continuation of our research work on pyridazinone , we have designed some hybrid benzimidolyl‐pyridazinone derivatives as anticonvulsant agents which possess all the essential pharmacophoric elements necessary for anticonvulsant activity .…”

Section: Introductionmentioning

confidence: 93%

Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

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Yar

Hassan

et al. 2017

Archiv der Pharmazie

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A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED values of 25.10 and 85.33 mg/kg in the MES and scPTZ screens, respectively. Compound SS-4F emerged as safer and effective anticonvulsant due to its several-fold higher protective indices. Further, the gamma-aminobutyric acid (GABA) estimation result showed a marked increase in the GABA level (1.7-fold) as compared to the control, which was further confirmed by good binding properties with the GABA receptor.

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Section: Introductionmentioning

confidence: 93%

Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

Partap

Yar

Hassan

et al. 2017

Archiv der Pharmazie

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“…Compound 522 at a dose of 2.34 mg/kg showed prominent anxiolytic, antidepressant and anticonvulsant activities in both rat and mice models. Vasil’ev et al ( Vasil’ev et al, 2017 ) investigated a series of imidazo[1,2-a]benzimidazole derivatives using corazole-induced seizure model. The compounds 523–526 displayed notable anticonvulsive activity in comparison with standard valproic acid.…”

Section: Biological Activitiesmentioning

confidence: 99%

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

et al. 2021

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Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world’s most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.

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“…Heterocyclic compounds play an important role in biochemistry, medicinal chemistry, organic chemistry and agrochemical industries. In recent years, attention has been given to the benzimidazole class of compounds due to their diverse biological activities, such as anticancer [1,2], antifungal [3], antioxidant [4], cytotoxic [5], antiprotozoal [6], anti-T. cruzi (Trypanosoma cruzi) [7], antiproliferative [8], antihistaminic [9], anti-inflammatory [10], analgesics [11], antibacterial [12], anticonvulsant [13] and acetylcholinesterase [14]. In addition, benzimidazole has been used as corrosion inhibition for mild steel [15], catalytic activity [16], fluorescence chemosensors [17] and chiroptical sensors [18].…”

Section: Introductionmentioning

confidence: 99%

Crystal Structure, Thermodynamic Properties and DFT Studies of 5,6-dimethyl-1H-benzo[d]imidazol-3-ium 3-((2,4-dioxo-1,5-dioxaspiro[5.5]undecan-3-ylidene)methyl) -2,4-dioxo-1,5-dioxaspiro[5.5]undecane Hydrate

2021

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A new 1,5-dioxaspiro[5.5] derivative coupled with a benzimidazole moiety: 5,6-dimethyl-1H-benzo[d]imidazol-3-ium 3-((2,4-dioxo-1,5-dioxaspiro[5.5]undecan-3-ylidene) methyl) -2,4-dioxo-1,5-dioxaspiro[5.5]undecane hydrate (DBH) was prepared. The crystal structure confirmed that it belongs to triclinic, P-1 space group. The title compound includes one (C19H21O8)− anion, one (C9H11N2)+ cation and one water molecule, which assembled into a 2D-net framework by O–H···O and N–H···O hydrogen bonds. The quantum chemical computations using the B3LYP/6-311G (d, p) basis level of theory reveal that the optimized geometric structure is suitable to study the molecule. The theoretically simulated FT-IR spectra and electronic spectra of DBH are compared with experimental data. The results show that the B3LYP/6-311g (d, p) method fits well with the molecular structure. In addition, the thermodynamic properties have also been studied to determine the nature of the DBH.

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Prediction and Study of Anticonvulsant Properties of Benzimidazole Derivatives

Cited by 20 publications

References 11 publications

Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Crystal Structure, Thermodynamic Properties and DFT Studies of 5,6-dimethyl-1H-benzo[d]imidazol-3-ium 3-((2,4-dioxo-1,5-dioxaspiro[5.5]undecan-3-ylidene)methyl) -2,4-dioxo-1,5-dioxaspiro[5.5]undecane Hydrate

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