In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives

Achar, Kavitha C. S.; Hosamani, Kallappa M.; Seetharamareddy, Harisha R.

doi:10.1016/j.ejmech.2010.01.029

Cited by 310 publications

(139 citation statements)

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“…Moreover, fused imidazole systems have attracted the researcher's interest due to their natural occurrence and significant medicinal applications [1][2][3]. Additionally, the benzimidazole derivatives are the bioisosters of natural nucleotides, which can interact easily with the macromolecules (proteins, enzymes and receptors) of the biological system, has made the benzimidazole and its derivatives as the privileged pharmacophore in drug discovery process [4,5].…”

Section: Introductionmentioning

confidence: 99%

Untitled

2017

MOJBOC

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Section: Introductionmentioning

confidence: 99%

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2017

MOJBOC

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“…Benzimidazole is an important pharmacophore and privileged structure in the field of medicinal chemistry because of its varied biological activities, viz., anticancer [8,9], antihypertensive [10,11], antiviral [12,13], anti-inflammatory [14,15], antihistaminic [16,17], antiulcer [18], anticoagulant [19,20], and antimicrobial [21,22]. The antimicrobial action of benzimidazole is due to its structural similarity to purines; therefore, its derivatives inhibit nucleic acid and protein synthesis by competing with natural purines; thereby inhibit the growth as well as kill bacterial strains [23].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and in Vitro Antimicrobial Evaluation of Some Novel Benzimidazole Derivatives Bearing Hydrazone Moiety

Sarma

Singh

Gupta

et al. 2017

Asian J Pharm Clin Res

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Objective: The synthesis of novel benzimidazole-hydrazone derivatives has been carried out based on the previous findings that both these pharmacophores possess potent antimicrobial activities. The antibacterial properties of synthesized derivatives were screened against both Grampositive and Gram-negative bacteria.Methods: O-phenylenediamine on condensation with substituted aromatic acids in polyphosphoric acid gave benzimidazole nucleus which on reaction with ethyl chloroacetate and hydrazine hydrate in two different steps resulted in the formation of substituted acetohydrazides. The targeted compounds 6a-l were synthesized by reaction of substituted acetohydrazides with aromatic aldehydes and screened for their antibacterial potential by cup-plate method. Results:The synthesized benzimidazole-hydrazones exhibited moderate to strong antibacterial activities against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. The compounds 6a-6f were found to be most effective against S. aureus, E. coli, and P. aeruginosa. Among all the synthesized compounds, the zone of inhibition of 6f in highest concentration, i.e., 100 µg/ml were found to be >31 mm against all the stains of bacteria. Conclusion:The antibacterial results revealed that the synthetized derivatives have significant antimicrobial properties and further structure activity relationship studies may develop more potent and less toxic molecules.

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“…Moreover, fused imidazole systems have attracted the researcher's interest due to their natural occurrence and significant medicinal applications. [1][2][3] Additionally, the benzimidazole derivatives are the bioisosters of natural nucleotides, which can interact easily with the macromolecules (proteins, enzymes and receptors) of the biological system, has made the benzimidazole and its derivatives as the privileged pharmacophore in drug discovery process. 4,5 They are able to produce anti-inflammatory, 6 antibacterial, 7 anti cancer, 8 analgesic , 9 antiviral 10 and anticonvulsant 11 activitie, etc., Further benzimidazoles also can act as inhibitors for α-Glucosidase, 12 Cyclooxygenase, 13 Poly (ADP-ribose) polymerase 14 and lysophosphatidic acid acyltransferase-β.…”

Section: Introductionmentioning

confidence: 99%

One-Pot Synthesis of a New Imidazole-5-Carboxylic Acid Derivative via Heterocyclization Reaction

Poojary¹

2017

MOJBOC

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In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives

Cited by 310 publications

References 29 publications

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Untitled

Synthesis, Characterization and in Vitro Antimicrobial Evaluation of Some Novel Benzimidazole Derivatives Bearing Hydrazone Moiety

One-Pot Synthesis of a New Imidazole-5-Carboxylic Acid Derivative via Heterocyclization Reaction

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