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◆ Chemistry & Biodiversity2026-02-01· Anticonvulsant

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

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

原始摘要(英文原文)· Original 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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Synthesis and Pd(0)‐Catalyzed Arylation of Naphthalen‐2‐yl 5‐Bromofuran‐2‐Carboxylate Derivatives: Anticonvulsant Evaluation via In Vivo and In Silico Studies — 科研速览 Science Skim