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February 19, 2026Chemistry & Biodiversity4 citationsOpen Access

Synthesis and Pd(0)‐Catalyzed Arylation of Naphthalen‐2‐yl 5‐Bromofuran‐2‐Carboxylate Derivatives: Anticonvulsant Evaluation via In Vivo and In Silico Studies

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BABisma AshrafNFNoor FatimaSKShehla Khalid

Key Points

  • This research aims to synthesize naphthalene derivatives and evaluate their anticonvulsant activity both in vivo and in silico.
  • Synthesis of naphthalene‐2‐yl 5‐bromofuran‐2‐carboxylate derivatives using palladium catalysis.
  • In vivo anticonvulsant testing with 6 Hz and pentylenetetrazol seizure models.
  • In silico molecular docking studies for GABA-A receptor and SV2A protein.
  • Assessment of compliance with Lipinski's rule of five and CNS penetration potential.
  • Compounds 5a and 5g showed anticonvulsant activity comparable to levetiracetam.
  • Molecular docking supported findings, indicating potential binding to GABA-A and SV2A.
  • All evaluated compounds complied with Lipinski's rule, suggesting good pharmacokinetic properties.

Abstract

ABSTRACT A series of naphthalene‐2‐yl 5‐bromofuran‐2‐carboxylate (5a–5h) was synthesized using a palladium‐catalyzed approach. The in vivo experiments and in silico studies were used to assess the anticonvulsant potential of the synthesized library of compounds. We tested the in vivo anticonvulsant activity using the acute 6 Hz model and pentylenetetrazol (PTZ) seizure models, antiepileptic potential of compounds 5a and 5g were comparable to the standard drug levetiracetam The molecular docking studies validated the in vivo experiment’ result showing that all 5a, 5g, 5b, 5e, and 5f are potential antiepileptic agents for the GABA‐A receptor and synaptic vesicle protein 2A (SV2A) protein, and their compliance to Lipinski's rule of five as well as their computed CNS penetration potential suggest their potential novel anticonvulsant properties.

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Cite This Study

Ashraf et al. (2026) studied this question.

synapsesocial.com/papers/6996a7c3ecb39a600b3edbddhttps://doi.org/10.1002/cbdv.202501490
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