Chimirri A, Grasso S, Monforte A M, Zappala M, De Sarro A, De Sarro G B
Dipartimento Farmaco-Chimico, Università di Messina, Italy.
Farmaco. 1991 Jul-Aug;46(7-8):935-43.
A series of 2-substituted 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-ones were synthesized and evaluated for anticonvulsant activity in a genetic model of reflex epilepsy (sound-induced seizures in DBA/2 mice). The combination of preferred substituents in the 2-position coupled with the introduction of a mercapto group on the thiadiazole moiety led to a number of active compounds. The anticonvulsant activity of most derivatives is better than that of the clinically useful anticonvulsant sodium valproate and some of them appear to possess potencies in the same range as phenytoin and clobazam.
合成了一系列2-取代的3-(1,3,4-噻二唑-2-基)噻唑烷-4-酮，并在反射性癫痫的遗传模型（DBA/2小鼠的声音诱发惊厥）中评估了其抗惊厥活性。2-位上优选取代基的组合以及在噻二唑部分引入巯基导致了许多活性化合物。大多数衍生物的抗惊厥活性优于临床上有用的抗惊厥药丙戊酸钠，其中一些似乎具有与苯妥英和氯巴占相同范围的效力。
