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Synthesis, molecular docking, antibacterial, and anti-inflammatory activities of benzimidazole-containing tricyclic systems

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F21%3A39917536" target="_blank" >RIV/00216275:25310/21:39917536 - isvavai.cz</a>

  • Result on the web

    <a href="https://www.researchgate.net/publication/348810368_Synthesis_molecular_docking_antibacterial_and_anti-inflammatory_activities_of_benzimidazole-containing_tricyclic_systems" target="_blank" >https://www.researchgate.net/publication/348810368_Synthesis_molecular_docking_antibacterial_and_anti-inflammatory_activities_of_benzimidazole-containing_tricyclic_systems</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1002/jccs.202000454" target="_blank" >10.1002/jccs.202000454</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Synthesis, molecular docking, antibacterial, and anti-inflammatory activities of benzimidazole-containing tricyclic systems

  • Original language description

    In the present study, we reported the synthesis of benzimidazole-containing tricyclic systems and evaluated their antimicrobial efficacy against some Gram-positive, Gram-negative strains, and their anti-inflammatory activity as well as a hemolytic assay in terms of percentage. The antimicrobial study of the synthesized compounds revealed that most of them showed significant activity, and compound 5b displayed excellent antimicrobial efficacy among all. Results showed that the hydroxyl group at the fourth position on the aromatic ring has a substantial role in the biological activity. Synthesized compounds showed promising minimum inhibitory concentration (mu g/mL) values in the range of 1.2-12.8 mu g/mL against the tested strains. The in vitro anti-inflammatory activity of these compounds was evaluated by denaturation of bovine serum albumin method and showed the inhibition in the range of IC50 value 31.16-94.63 mu g/mL. Among all the tested compounds, compound 5b has a significant IC50 value. The percentage of hemolysis of the target compounds ranged from 1.14 to 52.8 at a concentration of 100 mu g/mL. Molecular docking study revealed the good binding interactions against Escherichia coli, and it is best suited with in vitro studies. Pharmacokinetic studies showed the safe profiles for the title compounds.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    10401 - Organic chemistry

Result continuities

  • Project

  • Continuities

    S - Specificky vyzkum na vysokych skolach

Others

  • Publication year

    2021

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Journal of the Chinese Chemical Society

  • ISSN

    0009-4536

  • e-ISSN

  • Volume of the periodical

    68

  • Issue of the periodical within the volume

    6

  • Country of publishing house

    DE - GERMANY

  • Number of pages

    12

  • Pages from-to

    1055-1066

  • UT code for WoS article

    000612015400001

  • EID of the result in the Scopus database

    2-s2.0-85099796856