Thiry Anne, Dogné Jean-Michel, Supuran Claudiu T, Masereel Bernard
Drug Design and Discovery Center, FUNDP, University of Namur, 61 rue de Bruxelles, 5000 Namur, Belgium.
Curr Pharm Des. 2008;14(7):661-71. doi: 10.2174/138161208783877956.
The marketed antiepileptic drugs can not solve entirely the problem of seizure in patients suffering from refractory epilepsies. Therefore, new anticonvulsant compounds structurally and pharmacologically different of the currently prescribed drugs are needed. Carbonic anhydrase (CA) inhibitors are known to act as anticonvulsant since several decades while the link between CA and seizure is not straightforward. However, the recent discovery that several CA isozymes are expressed in brain and the better knowledge of their physiological/pathological role, lead to the emergence of new CA inhibitors with anticonvulsant effect including: analogues of acetazolamide, analogues of topiramate, aromatic or heterocyclic sulfonamides incorporating valproyl or adamantyl moieties. Different strategies are developed for the design of new more selective CA inhibitors with anticonvulsant properties.
市售的抗癫痫药物并不能完全解决难治性癫痫患者的癫痫发作问题。因此，需要结构和药理作用与目前处方药不同的新型抗惊厥化合物。几十年来，碳酸酐酶（CA）抑制剂一直被认为具有抗惊厥作用，而CA与癫痫发作之间的联系并不直接。然而，最近发现几种CA同工酶在大脑中表达，并且对它们的生理/病理作用有了更深入的了解，这导致了具有抗惊厥作用的新型CA抑制剂的出现，包括：乙酰唑胺类似物、托吡酯类似物、含有丙戊酰基或金刚烷基部分的芳香族或杂环磺酰胺。为设计具有抗惊厥特性的新型更具选择性的CA抑制剂，人们开发了不同的策略。
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