Neurotropic, Psychoactive, and Analgesic Properties of Benzimidazole and Its Derivatives: Physiological Mechanisms

Черетаев, И. В.; Korenyuk, I. I.; Nozdrachev, A. D.

doi:10.1007/s11055-018-0639-8

Cited by 7 publications

(5 citation statements)

References 11 publications

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“…Benzimidazole derivatives (substituted benzo[ d ]imidazol-1-yl)methyl)benzimidamides) were considered as potential analogues for AICAR due to similarities in chemical structure (Figure 1), and could be evaluated for their antimalarial propensity. Benzimidazole derivatives have been widely used in recent years due to their wide range of pharmacological activities including antimalarial, 8 antileishmanial, 9 analgesics, 10 anticancer, 11 antitumour, 12 antimicrobial, 13 anti-inflammatory, 14 antihepatitis C virus, 15 antihelmintic, 16 antibacterial 17 and antitrypanosomal 18 activities. Although several benzimidazole derivatives have been synthesised and developed into commercially available drugs, little is known about the design of the template as an inhibitor against P falciparum ADSL ( Pf ADSL).…”

Section: Introductionmentioning

confidence: 99%

Homology Modelling and Molecular Docking Studies of Selected Substituted Benzo[d]imidazol-1-yl)methyl)benzimidamide Scaffolds on Plasmodium falciparum Adenylosuccinate Lyase Receptor

Oduselu

Ajani

Ajamma

et al. 2019

Bioinform Biol Insights

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Plasmodium falciparum adenylosuccinate lyase ( PfADSL) is an important enzyme in purine metabolism. Although several benzimidazole derivatives have been commercially developed into drugs, the template design as inhibitor against PfADSL has not been fully explored. This study aims to model the 3-dimensional (3D) structure of PfADSL, design and predict in silico absorption, distribution, metabolism, excretion and toxicity (ADMET) of 8 substituted benzo[ d]imidazol-1-yl)methyl)benzimidamide compounds as well as predict the potential interaction modes and binding affinities of the designed ligands with the modelled PfADSL. PfADSL 3D structure was modelled using SWISS-MODEL, whereas the compounds were designed using ChemDraw Professional. ADMET predictions were done using OSIRIS Property Explorer and Swiss ADME, whereas molecular docking was done with AutoDock Tools. All designed compounds exhibited good in silico ADMET properties, hence can be considered safe for drug development. Binding energies ranged from −6.85 to −8.75 kcal/mol. Thus, they could be further synthesised and developed into active commercial antimalarial drugs.

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Section: Introductionmentioning

confidence: 99%

Homology Modelling and Molecular Docking Studies of Selected Substituted Benzo[d]imidazol-1-yl)methyl)benzimidamide Scaffolds on Plasmodium falciparum Adenylosuccinate Lyase Receptor

Oduselu

Ajani

Ajamma

et al. 2019

Bioinform Biol Insights

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“…Some benzimidazoles are efficient agents in Diabetes mellitus [25][26][27], while astemizole compounds possess anti-prion activity to treat Creutzfeldt-Jakob disease [5,28]. The literature also reports anti-Alzheimer [29,30], psychoactive, anxiolytic, analgesic [31,32], and anticoagulant properties [33,34] of benzimidazole derivatives.…”

Section: Introductionmentioning

confidence: 99%

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

Marinescu

2023

Antibiotics

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Bacterial infections have attracted the attention of researchers in recent decades, especially due to the special problems they have faced, such as their increasing diversity and resistance to antibiotic treatment. The emergence and development of the SARS-CoV-2 infection stimulated even more research to find new structures with antimicrobial and antiviral properties. Among the heterocyclic compounds with remarkable therapeutic properties, benzimidazoles, and triazoles stand out, possessing antimicrobial, antiviral, antitumor, anti-Alzheimer, anti-inflammatory, analgesic, antidiabetic, or anti-ulcer activities. In addition, the literature of the last decade reports benzimidazole-triazole hybrids with improved biological properties compared to the properties of simple mono-heterocyclic compounds. This review aims to provide an update on the synthesis methods of these hybrids, along with their antimicrobial and antiviral activities, as well as the structure–activity relationship reported in the literature. It was found that the presence of certain groups grafted onto the benzimidazole and/or triazole nuclei (-F, -Cl, -Br, -CF3, -NO2, -CN, -CHO, -OH, OCH3, COOCH3), as well as the presence of some heterocycles (pyridine, pyrimidine, thiazole, indole, isoxazole, thiadiazole, coumarin) increases the antimicrobial activity of benzimidazole-triazole hybrids. Also, the presence of the oxygen or sulfur atom in the bridge connecting the benzimidazole and triazole rings generally increases the antimicrobial activity of the hybrids. The literature mentions only benzimidazole-1,2,3-triazole hybrids with antiviral properties. Both for antimicrobial and antiviral hybrids, the presence of an additional triazole ring increases their biological activity, which is in agreement with the three-dimensional binding mode of compounds. This review summarizes the advances of benzimidazole triazole derivatives as potential antimicrobial and antiviral agents covering articles published from 2000 to 2023.

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“…Astemizole-related compounds demonstrated anti-prion activity for the treatment of Creutzfeldt–Jakob disease, while albendazole compounds are currently used as medication for the treatment of a variety of parasitic worm infestations. Additionally, benzimidazoles treat mitochondrial dysfunction in Alzheimer’s disease [ 22 ], possess neurotropic, psychoactive, analgesic effects [ 23 ], anticoagulant proprieties [ 24 ] and are efficient agents in Diabetes mellitus [ 25 ]. Additionally, pyrazole compounds possess a diversity of biological activities as analgesic [ 26 , 27 , 28 ], anticonvulsivant [ 29 , 30 ], antitumor [ 31 , 32 , 33 , 34 ], antidiabetic [ 35 , 36 ], antimicrobial [ 37 , 38 , 39 , 40 , 41 , 42 , 43 ], antipyretic [ 44 , 45 ], antiviral [ 46 , 47 ], antimalarial [ 48 , 49 ], local anesthetic [ 50 ] and so forth.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities

Marinescu

2021

Antibiotics

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The synthesis of new compounds with antimicrobial and antiviral properties is a central objective today in the context of the COVID-19 pandemic. Benzimidazole and pyrazole compounds have remarkable biological properties, such as antimicrobial, antiviral, antitumor, analgesic, anti-inflammatory, anti-Alzheimer’s, antiulcer, antidiabetic. Moreover, recent literature mentions the syntheses and antimicrobial properties of some benzimidazole–pyrazole hybrids, as well as other biological properties thereof. In this review, we aim to review the methods of synthesis of these hybrids, the antimicrobial activities of the compounds, their correlation with various groups present on the molecule, as well as their pharmaceutical properties.

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Neurotropic, Psychoactive, and Analgesic Properties of Benzimidazole and Its Derivatives: Physiological Mechanisms

Cited by 7 publications

References 11 publications

Homology Modelling and Molecular Docking Studies of Selected Substituted Benzo[d]imidazol-1-yl)methyl)benzimidamide Scaffolds on Plasmodium falciparum Adenylosuccinate Lyase Receptor

Homology Modelling and Molecular Docking Studies of Selected Substituted Benzo[d]imidazol-1-yl)methyl)benzimidamide Scaffolds on Plasmodium falciparum Adenylosuccinate Lyase Receptor

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

Synthesis of Antimicrobial Benzimidazole–Pyrazole Compounds and Their Biological Activities

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