Synthesis of methanesulphonamido-benzimidazole derivatives as gastro-sparing antiinflammatory agents with antioxidant effect

Sharma, Ruchi; Bali, Alka; Chaudhari, Bhim Bahadur

doi:10.1016/j.bmcl.2017.05.017

Cited by 38 publications

(23 citation statements)

References 22 publications

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“…In another study, Sharma et al (2017) evaluated methanesulphonamido-benzimidazoles for their gastro-sparing anti-inflammatory effects using a carrageenan-induced model of inflammation/oedema in rat hind paws. Compounds substituted with n-hexyl, n-pentyl and n-butyl at N1 of benzimidazole showed better anti-inflammatory activity (92.73, 95.64 and 97.62, maximum % reduction in oedema) than rofecoxib and indomethacin (78.95 and 75.00, maximum % reduction in oedema).…”

Section: Miscellaneousmentioning

confidence: 99%

Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview

et al. 2021

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A significant number of the anti-inflammatory drugs currently in use are becoming obsolete. These are exceptionally hazardous for long-term use because of their possible unfavourable impacts. Subsequently, in the ebb-and-flow decade, analysts and researchers are engaged in developing new anti-inflammatory drugs, and many such agents are in the later phases of clinical trials. Molecules with heterocyclic nuclei are similar to various natural antecedents, thus acquiring immense consideration from scientific experts and researchers. The arguably most adaptable heterocyclic cores are benzimidazoles containing nitrogen in a bicyclic scaffold. Numerous benzimidazole drugs are broadly used in the treatment of numerous diseases, showing promising therapeutic potential. Benzimidazole derivatives exert anti-inflammatory effects mainly by interacting with transient receptor potential vanilloid-1, cannabinoid receptors, bradykinin receptors, specific cytokines, 5-lipoxygenase activating protein and cyclooxygenase. Literature on structure–activity relationship (SAR) and investigations of benzimidazoles highlight that the substituent’s tendency and position on the benzimidazole ring significantly contribute to the anti-inflammatory activity. Reported SAR analyses indicate that substitution at the N1, C2, C5 and C6 positions of the benzimidazole scaffold greatly influence the anti-inflammatory activity. For example, benzimidazole substituted with anacardic acid on C2 inhibits COX-2, and 5-carboxamide or sulfamoyl or sulfonyl benzimidazole antagonises the cannabinoid receptor, whereas the C2 diarylamine and C3 carboxamide substitution of the benzimidazole scaffold result in antagonism of the bradykinin receptor. In this review, we examine the insights regarding the SARs of anti-inflammatory benzimidazole compounds, which will be helpful for researchers in designing and developing potential anti-inflammatory drugs to target inflammation-promoting enzymes.

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Section: Miscellaneousmentioning

confidence: 99%

Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview

et al. 2021

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“…Other benzimidazole derivatives has also shown remarkable in vitro antioxidant activity [18][19][20].…”

Section: Biological Activitymentioning

confidence: 99%

Synthesis and pharmacological screening of new isatin-3-[N2-(benzimidazol-1- acetyl)]hydrazone

Chaithanya¹,

Kasiviswanath²,

Chary³

2019

Bull. Chem. Soc. Eth.

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Twenty new isatin-3-[N 2 -(benzimidazol-1-acetyl)]hydrazones (IV) were synthesized from ten different isatin-3-[N 2 -(chloroacetyl)] hydrazones (III) by reacting with benzimidazole and 2-methyl benzimidazole. The intermediates were obtained from isatin hydrazones (II) on condensation with chloroacetyl chloride. These compounds were characterized by IR, 1 H NMR and mass spectra. All the compounds were screened for antimicrobial, antioxidant and cytotoxic activity. Some of the new compounds showed promising antibacterial and antifungal activity.

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“…Benzimidazolyl heterocycle is also considered for conjugation with the targeted compounds due to the diverse biological properties exhibited by its derivatives such as antitumor [24] , [25] , [26] , [27] , [28] , [29] , [30] , [31] , anti-inflammatory [32] , antitubercular [33] , [34] , [35] , anti-HIV (human immunodeficiency virus) [36] , [37] , [38] , α -glucosidase inhibition [39] , [40] , [41] , cholinesterase inhibitor useful to combat the neuromuscular disorders [42] , pancreatic lipase inhibitor useful for fat absorption control [43] , α -amylase inhibitor useful for diabetes, obesity, and oral diseases [44] and Rho-kinase inhibitor useful for treatment of glaucoma [45] . Treanda (Bendamustine hydrochloride) is a benzimidazolyl derivative approved by FDA (2008) for chronic lymphocytic leukemia [46] , [47] .…”

Section: Introductionmentioning

confidence: 99%

3-Alkenyl-2-oxindoles: Synthesis, antiproliferative and antiviral properties against SARS-CoV-2

Girgis

Panda

Srour

et al. 2021

Bioorganic Chemistry

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Synthesis of methanesulphonamido-benzimidazole derivatives as gastro-sparing antiinflammatory agents with antioxidant effect

Cited by 38 publications

References 22 publications

Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview

Structure–Activity Relationship Analysis of Benzimidazoles as Emerging Anti-Inflammatory Agents: An Overview

Synthesis and pharmacological screening of new isatin-3-[N2-(benzimidazol-1- acetyl)]hydrazone

3-Alkenyl-2-oxindoles: Synthesis, antiproliferative and antiviral properties against SARS-CoV-2

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