Design, Synthesis and Antibacterial Activity Evaluation of 4,5-Diphenyl-1&amp;lt;i&amp;gt;H&amp;lt;/i&amp;gt;-Imidazoles Derivatives

Bamoro, Coulibaly; Bamba, Fanté; Steve-Evanes, Koffi Téki Dindet; Vallin, Aurélie; Chagnault, Vincent

doi:10.4236/ojmc.2021.112002

Cited by 5 publications

(4 citation statements)

References 17 publications

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“…Tubulin inhibitors including methanone analogues, [14–15] colchicine, and indole‐based derivatives [16–17] are known to impart anticancer effects. Since our compounds exhibited anticancer activity in a number of cancer cell lines, we also conducted docking work on most potent anticancer compound 4 identified in this work [18–20] . Our work identifies new chemical groups and moieties that would help design and develop antidiabetic and anticancer drugs.…”

Section: Introductionmentioning

confidence: 97%

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Synthesis of Competitive and Noncompetitive Inhibitors of Alpha‐Glucosidase and Anticancer Agents

Ghani,

Syed,

Aljunidel

et al. 2024

Chemistry & Biodiversity

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Heterocyclic chemistry displays a broad range of applications in medicinal chemistry that offers convenient and efficient routes for the synthesis of biologically active heterocyclic compounds. Imidazoles and phenylthiazoles are an important class of heterocycles that demonstrate a wide range of biological activities against various types of cancers, diabetes mellitus and pathogenic microorganisms. The functionalization of the imidazole moiety at various positions makes it more potent and a versatile synthetic intermediate. Imidazole‐containing drugs bear multiple therapeutic applications in the treatment of various diseases. The heterocyclic structure having oxothiazolidine moiety is an important scaffold present in various drugs, with potential for enzyme inhibition. Furthermore, phenyl thiazoles are reported to be potent apoptosis inducers with potential anticancer activity. In an effort to identify these heterocyclic compounds, we synthesized 26 new 4,5‐diphenyl‐1H‐imidazole, phenylthiazole, and oxothiazolidine heterocyclic analogues, some of which demonstrated potent α‐glucosidase inhibition since the enzyme is an important clinical target for treatment of diabetes mellitus. Additionally, the analogues also exhibited significant activity against various types of cancers including non‐small lung cancer. Kinetics and molecular docking of the target compounds with α‐glucosidase and tubulin protein identified specific groups and moieties that bear importance for designing of new antidiabetic and anticancer drugs, respectively.

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Section: Introductionmentioning

confidence: 97%

“…Since our compounds exhibited anticancer activity in a number of cancer cell lines, we also conducted docking work on most potent anticancer compound 4 identified in this work. [18][19][20] Our work identifies new chemical groups and moieties that would help design and develop antidiabetic and anticancer drugs.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Competitive and Noncompetitive Inhibitors of Alpha‐Glucosidase and Anticancer Agents

Ghani,

Syed,

Aljunidel

et al. 2024

Chemistry & Biodiversity

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“…Imidazole derivatives are important and famous heterocyclic compound which shows the general and key structure of features of a variety of medicinal Pharmaceutical and natural products. Essential and synthetic imidazole derivatives occupy the main place among pharmaceutically and medicinally important compounds due to their different interesting and widespread medicinal Pharmaceutical and biological activity such as anti-oxidant [1][2] , antiviral [3][4] , anti-cancer [5][6] , anti-inflammatory [7][8] , antituberculosis [9][10] , anti-bacterial [11][12] , antifungal [13][14] , anti-diabetic [15][16] , anti-microbial [17][18] , anticonvulsant 19 , cytotoxic [20][21] , antiproliferative 22 , anticandidal 23 , antiamoebic 24 activity, etc.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2023

IJPSR

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A facile, highly efficient, simple, and convenient method for synthesizing 2, 4, 5-trisubstituted imidazole derivatives from the condensation of various substituted benzaldehyde, benzil, and ammonium acetate by using a catalytic amount of PEG-SOCl in the presence of water at room temperature or under microwave irradiation. PEG-SOCl is an effective heterogeneous catalyst and easy to separate. We have investigated that PEG-SOCl catalytic system was excellent recycled and reused three times without any loss of catalytic activity. PEG-SOCl act as a green catalyst, low-cost, non-volatile, non-hazardous, environmental friendly catalyst, and water is a green solvent reaction carried out at room temperature or under microwave radiation method shows greater advantages because it has contributed in the green chemistry aspects. The prepared catalyst was analyzed by analytical methods such as infrared spectrum (IR), X-Ray diffraction pattern (XRD), thermo-gravimetric analysis (TGA), and BET surface analysis. Spectroscopic techniques identified the synthesized pure product (1j), including infra-red (IR) spectrum, 1 H and 13 C NMR spectrum and Mass (LC-MS) spectrometry.

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“…Out of these heterocyclic compounds, imidazole and its derivatives have a wide variety of biological activities. [3][4][5][6][7][8] Imidazole is an important group of heterocyclic compounds that are biologically active and of significant importance in medicinal chemistry. The imidazole ring is an important pharmacophore in modern drug discovery.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization, In-Silico studies, and anti-inflammatory activity of Novel Imidazole-5(4H)-Ones

Muthuboopathi¹,

Shanmugarajan²

2022

ijhs

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Several new imidazole-5(4H)-one analog was synthesized using multi-step synthesis. All the synthesized compounds were characterized using FT-IR, 1H-NMR, Mass spectroscopy, and microanalysis to confirm their chemical structure. Molecular properties of the title compounds were predicted using Molinspiration online tool and binding studies of the title analogs against COX-1 & COX-2 were predicted by the molecular docking method. All novel imidazole-5(4H)-one analog were tested for their in-vivo anti-inflammatory activity using carrageenan-induced paw edema test in Wistar rats. Varying degree (weak to excellent) of anti-inflammatory activity was displayed by title compounds. In addition, in vitro anticancer potency of test compounds was estimated by the MTT assay method and found that most of the tested analogs were found to be inactive at 10 µM concentration against the tested cell lines. Among twelve tested title compounds, 2-methyl-1-(4-methyl piperazine-1-yl)-4-(naphthalen-1-ylmethylene)-1H-imidazol-5(4H)-one AL01, and 4-benzylidene-2-methyl-1-(4-methylpiperazin-1-yl)-1H-imidazol-5(4H)-one AL02 displayed more potent anti-inflammatory activity which is slightly higher than reference diclofenac.

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Design, Synthesis and Antibacterial Activity Evaluation of 4,5-Diphenyl-1<i>H</i>-Imidazoles Derivatives

Cited by 5 publications

References 17 publications

Synthesis of Competitive and Noncompetitive Inhibitors of Alpha‐Glucosidase and Anticancer Agents

Synthesis of Competitive and Noncompetitive Inhibitors of Alpha‐Glucosidase and Anticancer Agents

Untitled

Synthesis, characterization, In-Silico studies, and anti-inflammatory activity of Novel Imidazole-5(4H)-Ones

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