Pharmacological significance of heterocyclic 1H-benzimidazole scaffolds: a review

In the present study some substituted benzimidazole derivatives were screened for several biological activities. The synthesized compounds were subjected to evaluation of central analgesic, anti-inflammatory, cytotoxicity, antimicrobial and antioxidant activities by radiant heat induced tail flicking, carrageenan induced rat paw edema inhibition, brine shrimp lethality bioassay, disc diffusion and DPPH free radical scavenging methods, respectively. Compounds 2a, 2c and 2d elongated the tail flicking time by 58.07-, 51.59- and 76.65%, respectively (p < 0.001) at 50 mg/kg body weight dose compared to the standard morphine (87.17%). Compounds 2b, 2c and 2d showed prominent anti-inflammatory activity at 100 mg/kg body weight dose (% of paw edema inhibition 81.75%, 79.09% and 86.69%, respectively) compared to the standard aceclofenac (87.83%). Among the synthesized benzimidazole derivatives, compounds 1a, 1b, 1c, 2a and 2d exhibited potent cytotoxicity with the IC50 values of 5.47-, 11.92-, 4.55-, 7.63- and 7.94 μg/ml, respectively. In addition, compounds 1c and 2d displayed mild to moderate zone of inhibition (8-12 mm). On the other hand, 1a and 1b showed very mild antioxidant activity with IC50 values of 12.25 × 103 μg/ml and 87.33 ×103 μg/ml. Among all the derivatives, 2c, 2d and 1c can be potential candidates for designing new analgesic, anti-inflammatory and anti-cancer agents in future. Dhaka Univ. J. Pharm. Sci. 20(1): 95-102, 2021 (June)

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“…dabigatran 11 ; phosphodiesterase inhibitor, e.g. adibenden 9 ; antihypertensive, e.g. candesartan 12 ; anti-emetic, e.g.…”

Section: Introductionmentioning

confidence: 99%

Pharmacological Screening of Substituted Benzimidazole Derivatives

Saha

Brishty

Rahman

2021

Dhaka Univ. J. Pharm. Sci

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“…Benzimidazole is a vital pharmacophore in drug discovery. Benzimidazole-based drugs, such as albendazole, carbendazim, and tilomisole, are well exemplified [ 17 , 18 , 19 , 20 ]. Benzimidazole is one of the heterocyclic ring system components used to treat different types of cancer.…”

Section: Introductionmentioning

confidence: 99%

Ruthenium Complexes with 2-Pyridin-2-yl-1H-benzimidazole as Potential Antimicrobial Agents: Correlation between Chemical Properties and Anti-Biofilm Effects

Jabłońska-Wawrzycka

Rogala

Czerwonka

et al. 2021

IJMS

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Antimicrobial resistance is a growing public health concern that requires urgent action. Biofilm-associated resistance to antimicrobials begins at the attachment phase and increases as the biofilms maturate. Hence, interrupting the initial binding process of bacteria to surfaces is essential to effectively prevent biofilm-associated problems. Herein, we have evaluated the antibacterial and anti-biofilm activities of three ruthenium complexes in different oxidation states with 2-pyridin-2-yl-1H-benzimidazole (L1 = 2,2′-PyBIm): [(η6-p-cymene)RuIIClL1]PF6 (Ru(II) complex), mer-[RuIIICl3(CH3CN)L1]·L1·3H2O (Ru(III) complex), (H2L1)2[RuIIICl4(CH3CN)2]2[RuIVCl4(CH3CN)2]·2Cl·6H2O (Ru(III/IV) complex). The biological activity of the compounds was screened against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa strains. The results indicated that the anti-biofilm activity of the Ru complexes at concentration of 1 mM was better than that of the ligand alone against the P. aeruginosa PAO1. It means that ligand, in combination with ruthenium ion, shows a synergistic effect. The effect of the Ru complexes on cell surface properties was determined by the contact angle and zeta potential values. The electric and physical properties of the microbial surface are useful tools for the examined aggregation phenomenon and disruption of the adhesion. Considering that intermolecular interactions are important and largely define the functions of compounds, we examined interactions in the crystals of the Ru complexes using the Hirshfeld surface analysis.

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“…Moreover, the first effective therapy developed through benzimidazole moiety against the Ebola virus was an innovative breakthrough ( De Clercq, 2019 ). Categorically, several approved drugs derived from benzimidazole are currently available in the market and they can be grouped as 1 ) proton pump inhibitors (PPIs) exemplified by omeprazole, esomeprazole, lansoprazole, pantoprazole, etc., 2 ) anthelmintic drugs demonstrated by mebendazole, albendazole, oxibendazole, etc., 3 ) non-sedative H 1 -receptor blockers or antihistamine presented by astemizole, norastemizole, emedastine, mizolastine, etc., 4 ) angiotensin II receptor blocker illustrated by telmisartan, candesartan, azilsartan, and 5 ) calcium sensitized cardiac agents instanced by isomazole ( Tahlan et al, 2019 ).…”

Section: Expert Opinionmentioning

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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Pharmacological significance of heterocyclic 1H-benzimidazole scaffolds: a review

Cited by 119 publications

References 55 publications

Pharmacological Screening of Substituted Benzimidazole Derivatives

Pharmacological Screening of Substituted Benzimidazole Derivatives

Ruthenium Complexes with 2-Pyridin-2-yl-1H-benzimidazole as Potential Antimicrobial Agents: Correlation between Chemical Properties and Anti-Biofilm Effects

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

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