Abstract
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.
Highlights
Research the benzimidazole resulted in drugs such as alBenzimidazole is on bicyclic, comprising a nucleus benzenehas fused with an imidazole a fold exhibits anti-convulsant, antioxidant, anti-microbial, anticancer, anthelmin bendazole, mebendazole, thiabendazole, omeprazole, lansoprazole, pantoprazole, asteheteroaromatic compound with an amphoteric property (Figure 2)
The publications text and reduced to those dealing with benzimidazoles with anti-inflammatory action and were reviewed by title, abstract and text and reduced to those dealing with benzimidaztheir structure–activity relationships (SARs)
Benzimidazole derivatives act through different mechanisms, such as reducing cytokines, TRPV-1 antagonism, cannabinoid receptor agonism and FLAP inhibition
Summary
Reduction in activity of o-Cl group shows reduction in activity in activity shows potent. 24 of of 32 found that one of developed compounds, 2-(5-ethyl-2-pyridinyl)benzimidazole since thiabendazole hasthe moderate anti-inflammatory effects [62,63,64]. They found (KB-1043), better anti-inflammatory activity than phenylbutazone and (KB-1043), tiaramide. Acompound a 6-ethyl-2-pyridinyl moiety at the C2 position of elecbentron-withdrawing groups at C5 of benzimidazole resulted in a losselectron-withdrawing of anti-inflammatory zimidazole showed comparable activity to KB-1043. 62compounds and respectively, which is comparable toshowed the effect of dicloantiulcerogenic activity They electron-donating methoxy groups in that electron-donating methoxy groups in antiulcerogenic the pyrid-2-yl moiety mainly fenacshowed (73%). No substitution at R1, R2 and R3 activity results in least anti-inflammatory activity
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