Derivatives of benzimidazole pharmacophore: Synthesis, anticonvulsant, antidiabetic and DNA cleavage studies

Shingalapur, Ramya V.; Hosamani, Kallappa M.; Keri, Rangappa S.; Hugar, Mallinath H.

doi:10.1016/j.ejmech.2010.01.007

Cited by 224 publications

(109 citation statements)

References 25 publications

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“…Well versed with the intrinsic antimicrobial property of sulphur, 1H-2-mercapto benzimidazole 1 was aptly used as the starting material to incorporate 1H-benzimidazol-2-ylthio methyl motif into the target molecules. 2-(1-H-benzo[d] imidazol-2ylthio) acetic acid 2 was obtained through William's reaction of 1 with chloroacetic acid in the presence of sodium hydroxide [8,25] . On treatment with thionyl chloride, 2 yielded the acid chloride, 2-(1-H-benzo[d]imidazol-2ylthio)acetyl chloride 3 [26,27] .…”

Section: Resultsmentioning

confidence: 99%

“…Being structural surrogates of nucleotides, benzimidazole derivatives exhibited the potential to interact with proteins, enzymes and receptors. Substituted benzimidazoles were found to possess various biological activities such as antibacterial [3] , antiinflammatory [4] , antifungal [5] , antitubercular [6] , anticancer [7] , anticonvulsant and antidiabetic [8] . A number of 2-thio-1H-benzimidazole derivatives have been demonstrated to exhibit potent antiparasitic [9,10] activities.…”

Section: Research Papermentioning

confidence: 99%

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Synthesis, Spectral Characterization and Antimicrobial Studies of New Hybrid Heterocyclic Compounds Bearing 1H-benzimidazol-2-yl Thiomethyl Motif

Deshp¹,

Chavan²,

Nagarale³

et al. 2017

pharmaceutical-sciences

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Deshpande, et al.: Compounds with 1H-benzimidazol-2-yl Thiomethyl MotifTo understand the biological importance of heterocyclic cores, novel 1H-benzimidazol-2-yl thiomethyl incorporated hybrid compounds, 2-(benzimidazol-2-ylthiomethyl)-5-aryl-1,3,4-oxadizoles and 1-(2-(1H-benzo[d]imidazol-2-ylthio)acetyl)pyridazine/phthalazinediones were designed using molecular hybridization technique, synthesized and characterized. The compounds were screened for in vitro antimicrobial activity using the serial dilution technique and were found to exhibit weak antitubercular activity, excellent to moderate antibacterial and better antifungal activities against some tested organisms in comparison to the standard drugs. Thus, some of the title compounds demonstrated antimicrobial activity.

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Section: Resultsmentioning

confidence: 99%

Section: Research Papermentioning

confidence: 99%

Synthesis, Spectral Characterization and Antimicrobial Studies of New Hybrid Heterocyclic Compounds Bearing 1H-benzimidazol-2-yl Thiomethyl Motif

Deshp¹,

Chavan²,

Nagarale³

et al. 2017

pharmaceutical-sciences

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“…Many effects have been found, including anti-inflammatory and analgesic [15], antitubercular [16], antimicrobial and antifungal [17], antiviral, especially as anti-HIV agents [18], anticancer, antioxidants [19], anticonvulsants [20] and antidiabetic activity [21]. In the present study, some new derivatives of ibuprofen that contain thiazolidine-4-one scaffolds were synthesized in order to obtain compounds with double effect-antioxidant and anti-inflammatory properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of New 1,3-Thiazolidine-4-one Derivatives of 2-(4-Isobutylphenyl)propionic Acid

et al. 2014

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New thiazolidine-4-one derivatives of 2-(4-isobutylphenyl)propionic acid (ibuprofen) have been synthesized as potential anti-inflammatory drugs. The structure of the new compounds was proved using spectral methods (FR-IR, 1 H-NMR, 13 C-NMR, MS). The in vitro antioxidant potential of the synthesized compounds was evaluated according to the total antioxidant activity, the DPPH and ABTS radical scavenging assays. Reactive oxygen species (ROS) and free radicals are considered to be involved in many pathological events like diabetes mellitus, neurodegenerative diseases, cancer, infections and more recently, in inflammation. It is known that overproduction of free radicals may initiate and amplify the inflammatory process via upregulation of genes involved in the production of proinflammatory cytokines and adhesion molecules. The chemical modulation of acyl hydrazones of ibuprofen 3a-l through cyclization to the corresponding thiazolidine-4-ones 4a-n led to increased antioxidant potential, as all thiazolidine-4-ones were more active than their parent acyl hydrazones and also ibuprofen. The most active compounds are the thiazolidine-4-ones 4e, m, which showed the highest DPPH radical scavenging ability, their activity being comparable with vitamin E.

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“…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]. This vast applicability and usefulness of the fused imidazole nucleus inspired us to design and develop the target molecule.…”

Section: Introductionmentioning

confidence: 99%

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Derivatives of benzimidazole pharmacophore: Synthesis, anticonvulsant, antidiabetic and DNA cleavage studies

Cited by 224 publications

References 25 publications

Synthesis, Spectral Characterization and Antimicrobial Studies of New Hybrid Heterocyclic Compounds Bearing 1H-benzimidazol-2-yl Thiomethyl Motif

Synthesis, Spectral Characterization and Antimicrobial Studies of New Hybrid Heterocyclic Compounds Bearing 1H-benzimidazol-2-yl Thiomethyl Motif

Synthesis and Biological Evaluation of New 1,3-Thiazolidine-4-one Derivatives of 2-(4-Isobutylphenyl)propionic Acid

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