A search of novel antimicrobial based on benzimidazole and 2-pyridone heterocycles

Desai, N. C.; Dodiya, Amit M.; Shihory, Niraj

doi:10.1007/s00044-011-9782-2

Cited by 20 publications

(9 citation statements)

References 23 publications

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“…Benzimidazoles are found to be useful intermediates for the development of new molecules of biological or pharmaceutical interest. Substituted benzimidazole derivatives have been found to possess Biological activities such as antitumor [1], antimicrobial [2], anthelmintic [3], antibacterial [4], analgesic [5], anti inflammatory [6] etc. In recent times, new techniques have been adopted for the efficient synthesis of novel heterocycles by using heterogeneous, nano-catalysts and photocatalysis that are highly and ecofriendly [7][8][9][10][11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, antibacterial and molecular docking studies of new benzimidazole derivatives

Gullapelli¹,

Brahmeshwari

Ravichander³

et al. 2017

Egyptian Journal of Basic and Applied Sciences

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a b s t r a c tThe new analogs of benzimidazole fused heterocyclic compounds such as triazinane and oxadiazinanes were synthesised by classical amino methylation with different aryl-N,N 0 unsymmetrical thioureas. The antibacterial activity of triazinane and oxadiazinane compounds have been assessed with zone of inhibition by well diffusion method using a panel of selected gram positive and gram negative bacterial strains and which have showed good activity. The synthesised molecules were subjected to molecular docking studies with two proteins, namely topoisomerase II (PDB ID: 1JIJ) and DNA gyrase subunit b (PDB ID : 1KZN). The molecular docking studies are supporting the antibacterial activity exhibiting high inhibition constant and binding energy. Ó 2017 Mansoura University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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Section: Introductionmentioning

confidence: 99%

Synthesis, antibacterial and molecular docking studies of new benzimidazole derivatives

Gullapelli¹,

Brahmeshwari

Ravichander³

et al. 2017

Egyptian Journal of Basic and Applied Sciences

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“…The therapeutic and pharmacological properties of pyridone heterocycles make them candidates of contemporary choice for use in diverse applications such as antimicrobial, anticancer or antitumoral, antiviral, anti‐inflammatory, etc. Antimicrobial potential of 2‐pyridone heterocyclic compounds has been extensively studied and documented . Such structures are part of many naturally occurring alkaloids and have been reported to possess broad‐spectrum therapeutic potential .…”

Section: Introductionmentioning

confidence: 99%

“…In view of the above considerations, a new bio‐inspired polymer having a 2‐pyridone structure was synthesized, namely poly(4‐vinyl‐2‐pyridone) (p‐VPn). It has a cyclic amide structure similar to the ones mentioned above . p‐VPn was further functionalized to its N ‐alkylated cationic derivative, poly( N ‐hydroxyethyl)‐4‐vinyl‐2‐pyridonium chloride (p‐HEVPnCl), to obtain a choline analogous polymeric structure with pendant —CH 2 CH 2 OH groups.…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial properties of bio-inspired poly(4-vinyl-2-pyridone) and itsN-alkylated cationic derivatives

2016

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Developing new antimicrobial polymers and designing new antimicrobial materials are important research areas for overcoming bacterial resistance. In the present study a new polymer, poly(4-vinyl-2-pyridone), having bioactive structure analogous to that of naturally occurring heterocyclic compounds, was synthesized from 4-vinylpyridine following a simple protocol. To augment the antibacterial properties of the synthesized polymer, N-alkylation of the heterocyclic pyridone moieties was achieved with ethylene chlorohydrin (2-chloroethanol) to generate choline analogous structure. Also, its N-butylated analogue was synthesized as a reference compound to study structure-activity relationship. Structures of the polymers were confirmed using various characterization techniques. Antimicrobial efficacy of the polymers was determined using the minimum inhibitory concentration method in parallel experiments. The test microorganisms used were a Gram (+) bacterium (Staphylococcus epidermidis), Gram (−) bacteria (Salmonella typhi, Pseudomonas aeruginosa and Escherichia coli) and a fungus (Candida albicans). Both the polymer derivatives are far more effective antimicrobial agents than the pristine polymer. Trends in the antimicrobial efficacy of these polymers correlate with their zeta potential values.

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“…1 . Some of these compounds are in preclinical testing while others are still in the early laboratory investigation phase, for example, FB642 [ 15 – 17 ], A-62022 [ 18 ], Hoechst-33258 [ 19 , 20 ], Nocodazole (NSC-238189) [ 21 , 22 ], and ABT-888 (Veliparib). The latter is a potential antitumor drug.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antiproliferative Activities of Benzimidazole-Based Sulfide and Sulfoxide Derivatives

Gaballah

El‐Nezhawy

Amer³

et al. 2016

Sci. Pharm.

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The design, synthesis, and in vitro antiproliferative activity of a novel series of sulfide (4a–i) and sulfoxide (5a–h) derivatives of benzimidazole, in which different aromatic and heteroaromatic acetamides are linked to benzimidazole via sulfide (4a–i) and sulfoxide (5a–h) linker, are reported and the structure-activity relationship is discussed. The new derivatives were prepared by coupling 2-(mercaptomethyl)benzimidazole with 2-bromo-N-(substituted) acetamides in dry acetone in the presence of anhydrous potassium carbonate. With very few exceptions, all of the synthesized compounds showed varying antiprolific activities against HepG2, MCF-7, and A549 cell lines. Compound 5a was very similar in potency to doxorubicin as an anticancer drug, with IC50 values 4.1 ± 0.5, 4.1 ± 0.5, and 5.0 ± 0.6 µg/mL versus 4.2 ± 0.5, 4.9 ± 0.6, and 6.1 ± 0.6 µg/mL against HepG2, MCF-7, and A549 cell lines, respectively. In contrast, none of the compounds showed activity against human prostate PC3 cancer cells. Additionally, the sulfoxide derivatives were more potent than the corresponding sulfides.

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A search of novel antimicrobial based on benzimidazole and 2-pyridone heterocycles

Cited by 20 publications

References 23 publications

Synthesis, antibacterial and molecular docking studies of new benzimidazole derivatives

Synthesis, antibacterial and molecular docking studies of new benzimidazole derivatives

Antimicrobial properties of bio-inspired poly(4-vinyl-2-pyridone) and itsN-alkylated cationic derivatives

Synthesis and Antiproliferative Activities of Benzimidazole-Based Sulfide and Sulfoxide Derivatives

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