Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines

doi:10.3109/14756366.2014.899593

Paper

Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines

Published Mar 4, 2015 · M. O. Püsküllü, S. Yıldız, Y. Duydu

Journal of Enzyme Inhibition and Medicinal Chemistry

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Abstract

Abstract A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines (23–33) have been synthesized and evaluated for their potential antistaphylococcal activity. Cytotoxic effects of the compounds were investigated by the neutral red uptake (NRU) cytotoxicity test. Most of the compounds exhibited good MICs values against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Compound 28 with N-cyclohexylcarboxamidine group at the 5-position was found to be the most potent agent, with the MIC value of 3.12 µg/mL.

In Vitro Study

Study Snapshot

New 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines show potent antistaphylococcal activity, with compound 28 being the most potent against Staphyloc

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines

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References

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N-substituted benzimidazole-sulfonamides show promising antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus, with compounds 30, 31, and 32 showing the lowest MIC values.

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The synthesized compounds show promising in vitro activity against various parasites and fungi, with superior activity against Plasmodium falciparum compared to chloroquine.

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Synthesis and Potent Antimicrobial Activities of Some Novel Retinoidal Monocationic Benzimidazoles

Novel retinoidal monocationic benzimidazoles show potent antibacterial and antifungal activities against S. aureus, MRSA, C. albicans, and C. krusei, with MIC values comparable to Fluconazole and Sultamicillin.

Synthesis and Potent Antimicrobial Activity of Some Novel N-(Alkyl)-2-Phenyl-1H-Benzimidazole-5-Carboxamidines

Novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidine derivatives show potent antibacterial and antifungal activity against various bacteria and fungi.

Citations

1H-Benzimidazole-5-carboxamidine derivatives: design, synthesis, molecular docking, DFT and antimicrobial studies

New 1H-benzimidazole-5-carboxamidine derivatives show significant efficacy against MRSA and VREF, with potential as new antimicrobial agents.

New method for the synthesis of 2-substituted benzimidazole-5(6)-carboxylic acids

This study presents a new method for synthesizing 2-substituted benzimidazole-5(6)-carboxylic acids using acid-catalyzed rearrangement of 2(3)-aroyl-3(2)-oxo-3,4(1,2)-dihydroquinoxa

Synthesis and In Vitro Activity of Polyhalogenated 2‐phenylbenzimidazoles as a New Class of anti‐MRSA and Anti‐VRE Agents

Polyhalogenated 2'-phenylbenzimidazoles show potential as a new class of potent anti-methicillin-resistant Staphylococcus aureus and anti-vancomycin-resistant Enterococcus faecium agents.

Synthesis and potent cytotoxicity of some novel imidazopyridine derivatives against MCF-7 human breast adenocarcinoma cell line

Novel imidazopyridine derivatives show high cytotoxic activity against MCF-7 breast cancer cells, with N-Hydroxy-4-(3H-imidazo[4,5-b]pyridin-2-yl)benzenecarboximidamide showing the most activity.

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