两种具有抗惊厥活性的新型3-氨基-5-[4-氯-2-苯氧基苯基]-4H-1,2,4-三唑的合成

Mahdavi Mohammad, Akbarzadeh Tahmineh, Sheibani Vahid, Abbasi Maryam, Firoozpour Loghman, Tabatabai Sayyed Abbas, Shafiee Abbas, Foroumadi Alireza

Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.

Kerman Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran.

Iran J Pharm Res. 2010 Summer;9(3):265-9.

Two novel 3-amino-5-(4-choloro-2-phenoxyphenyl)-4H-1,2,4-triazole derivatives were prepared and their anticonvulsant activity was measured by evaluation of the ability of these compounds to protect mice against convulsion induced by lethal doses of pentylenetetrazole (PTZ). Diazepam (Sigma) was considered as a positive control drug with anticonvulsant effect [ED50 = 1.2 (0.5-1.9) mg/Kg]. Amongst the compounds tested, compound 3, 3-amino-5- [4-chloro-2-(2-flurophenoxy)phenyl]-4H-1,2,4-triazole, showed potent anticonvulsant activity [ED50 = 1.4 (1.0-2.2) mg/Kg] compared to diazepam.

制备了两种新型的3-氨基-5-(4-氯-2-苯氧基苯基)-4H-1,2,4-三唑衍生物，并通过评估这些化合物保护小鼠免受致死剂量戊四氮(PTZ)诱导惊厥的能力来测定它们的抗惊厥活性。地西泮（Sigma）被视为具有抗惊厥作用的阳性对照药物[半数有效剂量（ED50）=1.2（0.5 - 1.9）mg/Kg]。在所测试的化合物中，化合物3，即3-氨基-5-[4-氯-2-(2-氟苯氧基)苯基]-4H-1,2,4-三唑，与地西泮相比显示出强效的抗惊厥活性[ED50 = 1.4（1.0 - 2.2）mg/Kg]。