Design, synthesis and antibacterial activity of novel actinonin derivatives containing benzimidazole heterocycles

Zhang, Datong; Wang, Zong-Heng; Xu, Weifeng; Sun, Feifei; Li-da, Tang; Wang, Jianwu

doi:10.1016/j.ejmech.2008.05.009

Cited by 41 publications

(31 citation statements)

References 14 publications

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“…[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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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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“…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 [15]. Interestingly, benzimidazoles are also being incorporated into various commercially available drugs [16,17].…”

Section: Introductionmentioning

confidence: 99%

Untitled

2017

MOJBOC

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“…One way to counteract the challenge of microbial resistance is judicious use of currently available antibiotics; the other is the development of new anti-ineffective agents with enhanced activity and a novel mechanism of action [5,6]. The bacteria exhibit phenotypic resistance, i.e., tolerance, rendering them to 1000-fold more resistant to commercially available antibiotics, is due to their ability to grow in sessile or adherent state which leads to formation of biofilms [7].…”

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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Design, synthesis and antibacterial activity of novel actinonin derivatives containing benzimidazole heterocycles

Cited by 41 publications

References 14 publications

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

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

Untitled

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

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