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September 5, 2025ScienceRise Pharmaceutical ScienceOpen Access

Bioisosteric replacement in the search for antimicrobial agents: design, synthesis and activity of novel 6-(1h-Benzimidazol-2-yl)-1-alkyl-3,5-dimethylthieno2,3-dpyrimidine-2,4(1h,3h)-dione derivatives

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Authors

OVOlena VlasovaSVSergiy V. VlasovHSHanna Severina

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Overview

Molecular docking revealed binding to TrmD in bacterial enzymes, suggesting enhanced biofilm disruption by new benzimidazole-thienopyrimidine hybrids.

Key Points

  • Bioisosteric modification led to synthesized compounds with significant antimicrobial activity.
  • Compound 5c exhibited the highest activity against both Gram-positive and Gram-negative bacterial strains.
  • Molecular docking confirmed a hydrogen bond formation between the synthesized compounds and the TrmD enzyme.
  • Bioisosteric hybrids demonstrated effective biofilm disruption, highlighting their potential for development as antimicrobial agents.

Cite This Study

Vlasova et al. (2025) studied this question.

synapsesocial.com/papers/68c239a3b210217d6477ce55https://doi.org/10.15587/2519-4852.2025.334881
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