Design, synthesis and anticonvulsant activity of new imidazolidindione and imidazole derivatives

Marzouk, Adel A.; Bass, Amr K.A.; Ahmed, Montaser Sh.; Abdelhamid, Antar A.; Elshaier, Yaseen A.M.M.; Salman, Asmaa; Aly, Omar M.

doi:10.1016/j.bioorg.2020.104020

Cited by 29 publications

(18 citation statements)

References 28 publications

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“…Continuing our quest to find a compound with improved antimicrobial properties [ 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 ], the current study describes the synthesis and structure elucidation of Fluoroquinolone(ciprofloxacin)-based hybrids containing various heterocycle derivatives, as well as antimicrobial activity evaluation using various strains of Gram-positive ( S. aureus and B. subtilis ), Gram-negative ( E. coli and P. aeruginosa ), and fungi ( A. flavus and C. albicans ). In addition, the inhibitory activity of the most active compounds against E. coli DNA gyrase and topoisomerase IV has been identified as a potential molecular target.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors

et al. 2021

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A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using 1H NMR, 13C NMR, and elementary analyses. Using ciprofloxacin as a reference, compounds 1–21 were screened in vitro against Gram-positive bacterial strains such as Staphylococcus aureus and Bacillus subtilis and Gram-negative strains such as Escherichia coli and Pseudomonas aeruginosa. As a result, many of the compounds examined had antibacterial activity equivalent to ciprofloxacin against test bacteria. Compounds 2–6, oxadiazole derivatives, were found to have antibacterial activity that was 88 to 120% that of ciprofloxacin against Gram-positive and Gram-negative bacteria. The findings showed that none of the compounds tested had antifungal activity against Aspergillus flavus, but did have poor activity against Candida albicans, ranging from 23% to 33% of fluconazole, with compound 3 being the most active (33% of fluconazole). The most potent compounds, 3, 4, 5, and 6, displayed an IC50 of 86, 42, 92, and 180 nM against E. coli DNA gyrase, respectively (novobiocin, IC50 = 170 nM). Compounds 4, 5, and 6 showed IC50 values (1.47, 6.80, and 8.92 µM, respectively) against E. coli topo IV in comparison to novobiocin (IC50 = 11 µM).

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors

et al. 2021

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“…More importantly, the tested compounds may have different therapeutic activities in different models. Thus, the model discrepancy should be considered when evaluating the tested drugs [ 22 ].…”

Section: Generalized Tonic-clonic Seizure Modelsmentioning

confidence: 99%

Animal Models of Epilepsy: A Phenotype-oriented Review

Wang¹,

Wei²,

Feng³

et al. 2022

Aging and disease

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Epilepsy is a serious neurological disorder characterized by abnormal, recurrent, and synchronous discharges in the brain. Long-term recurrent seizure attacks can cause serious damage to brain function, which is usually observed in patients with temporal lobe epilepsy. Controlling seizure attacks is vital for the treatment and prognosis of epilepsy. Animal models, such as the kindling model, which was the most widely used model in the past, allow the understanding of the potential epileptogenic mechanisms and selection of antiepileptic drugs. In recent years, various animal models of epilepsy have been established to mimic different seizure types, without clear merits and demerits. Accordingly, this review provides a summary of the views mentioned above, aiming to provide a reference for animal model selection.

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“…Imidazole derivatives are important and famous heterocyclic compound which shows the general and key structure of features of a variety of medicinal Pharmaceutical and natural products. Essential and synthetic imidazole derivatives occupy the main place among pharmaceutically and medicinally important compounds due to their different interesting and widespread medicinal Pharmaceutical and biological activity such as anti-oxidant [1][2] , antiviral [3][4] , anti-cancer [5][6] , anti-inflammatory [7][8] , antituberculosis [9][10] , anti-bacterial [11][12] , antifungal [13][14] , anti-diabetic [15][16] , anti-microbial [17][18] , anticonvulsant 19 , cytotoxic [20][21] , antiproliferative 22 , anticandidal 23 , antiamoebic 24 activity, etc.…”

Section: Introductionmentioning

confidence: 99%

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2023

IJPSR

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A facile, highly efficient, simple, and convenient method for synthesizing 2, 4, 5-trisubstituted imidazole derivatives from the condensation of various substituted benzaldehyde, benzil, and ammonium acetate by using a catalytic amount of PEG-SOCl in the presence of water at room temperature or under microwave irradiation. PEG-SOCl is an effective heterogeneous catalyst and easy to separate. We have investigated that PEG-SOCl catalytic system was excellent recycled and reused three times without any loss of catalytic activity. PEG-SOCl act as a green catalyst, low-cost, non-volatile, non-hazardous, environmental friendly catalyst, and water is a green solvent reaction carried out at room temperature or under microwave radiation method shows greater advantages because it has contributed in the green chemistry aspects. The prepared catalyst was analyzed by analytical methods such as infrared spectrum (IR), X-Ray diffraction pattern (XRD), thermo-gravimetric analysis (TGA), and BET surface analysis. Spectroscopic techniques identified the synthesized pure product (1j), including infra-red (IR) spectrum, 1 H and 13 C NMR spectrum and Mass (LC-MS) spectrometry.

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Design, synthesis and anticonvulsant activity of new imidazolidindione and imidazole derivatives

Cited by 29 publications

References 28 publications

Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors

Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors

Animal Models of Epilepsy: A Phenotype-oriented Review

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