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

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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Journal
Chemistry & Biodiversity
Published
2026-02-01
DOI
https://doi.org/10.1002/cbdv.202501490
Primary Topic
Catalytic Cross-Coupling Reactions
Type
article
Field-Weighted Citation Impact
0.00

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article

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

Aqsa Kanwal, Farhan Siddique, Bisma Ashraf, Noor Fatima et al.
Chemistry & Biodiversity
Catalytic Cross-Coupling Reactions
article

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

Aqsa Kanwal, Farhan Siddique, Bisma Ashraf, Noor Fatima, Imran Imran, Shehla Khalid, Nasir Rasool, Muhammad Imran, Muhammad Iftikhar Shoukat
article en

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.

Chemistry & BiodiversityVol. 23(2)
Bahauddin Zakariya University (PK), Government College University, Faisalabad (PK), King Khalid University (SA)
Council of Scientific and Industrial Research, India
Openalex Percentile: Top 52%
Catalytic Cross-Coupling Reactions
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