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Synthesis and anticonvulsant activity of aromatic tetramethylcyclopropanecarboxamide derivatives.

Abstract：

:As part of our ongoing research on potential new antiepileptic drugs (AEDs), a series of tetramethylcyclopropanecarboxamide derivatives containing benzene ring were designed, synthesized, and evaluated for anticonvulsant activities in the murine maximal electroshock (MES) and subcutaneous pentylenetetrazole (scMet) seizure tests. The most potent compound emerging from this study was N-(2,2,3,3-tetramethylcyclopropanecarboxamide)-p-phenyl-sulfonamide (21), possessing an ED(50) value of 26mg/kg in the rat-MES test and a remarkable PI (PI=TD(50)/ED(50)) value above 19. The better anticonvulsant potency of compound 21 and its wider safety margin compared to valproic acid (VPA) and zonisamide make it a potential candidate to become a new AED second-generation to VPA.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Shimshoni JA,Bialer M,Yagen B

doi

10.1016/j.bmc.2008.03.051

subject

Has Abstract

pub_date

2008-06-01 00:00:00

pages

6297-305

issue

11

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00276-9

journal_volume

16

pub_type

杂志文章

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