De Sarro A, De Sarro G, Gitto R, Grasso S, Micale N, Quartarone S, Zappalà M
Istituto di Farmacologia, Facoltà di Medicina, Università di Messina, Italy.
Bioorg Med Chem Lett. 1998 Apr 21;8(8):971-6. doi: 10.1016/s0960-894x(98)00148-6.
The synthesis and anticonvulsant activity of novel 7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones 3a-e, structurally-related to GYKI 52466 1, a well-known noncompetitive AMPA-receptor antagonist, are reported. The new compounds possess marked anticonvulsant properties and, in analogy to 1, antagonize seizures induced by AMPA. In addition, when compared to the model compound 1, compounds 3 show a longer-lasting anticonvulsant activity and a lower toxicity.
报道了新型7,8-亚甲基二氧基-4H-2,3-苯并二氮杂卓-4-酮3a-e的合成及其抗惊厥活性，这些化合物在结构上与著名的非竞争性AMPA受体拮抗剂GYKI 52466 1相关。新化合物具有显著的抗惊厥特性，并且与1类似，可拮抗由AMPA诱导的癫痫发作。此外，与模型化合物1相比，化合物3显示出更持久的抗惊厥活性和更低的毒性。
