Synthesis and Research Anticonvulsant Activity of Annulated Triazolo-Thiadiazine Derivative in Laboratory Animals
Zafar Isomiddinovich Sanoev1,2
, Dilnoza Safaralievna Ismailova3, Sukhrob Davlatyor ogli Rakhimboev1, Tolmas Tolibovich Khamroev1, Burkhon Zhuraevich Elmuradov3, Ibrokhimjon Tuychievich Abdinazar1 and Sokhib Zamon ogli Rashidov11Department of pharmacology and toxicology of the Institute of Chemistry of Plant Substances named after Academician S.Yu. Yunusov of the Academy of Sciences of the Republic of Uzbekistan, 100170, Mirzo-Ulugbek str., 77, Tashkent, Uzbekistan.
2Department microbiology and pharmacology of Tashkent State Dental Institute, 100047, Yashnobod dist., Taraqqiyot str., 103, Tashkent, Uzbekistan,
3Department of Organic synthesis of the Institute of Chemistry of Plant Substances named after Academician S.Yu. Yunusov of the Academy of Sciences of the Republic of Uzbekistan, 100170, Mirzo-Ulugbek str., 77, Tashkent, Uzbekistan.
Corresponding Author E-mail: zafarsano19@mail.ru
Abstract: Epilepsy is a chronic non-communicable disease of the brain, which is estimated that five million people are diagnosed with epilepsy every year worldwide. In this regard the study studied the anticonvulsant properties of annulated 4-(6-phenyl-7H-[1,2,4] triazolo [3,4-b] [1,3,4] thiadiazin-3-yl)-aniline. Anticonvulsant activity was evaluated in various experimental models of convulsions in laboratory rodents. Oral dosages of 3, 10, 30, and 60 mg/kg of the study substances were given one hour prior to the experiment. Pentylenetetrazole (PTZ) convulsions were modeled using PTZ at a dose of 7 mg/kg subcutaneously, isoniazid convulsions were modeled using an oral dose of 300 mg/kg, and bicuculline convulsions were modeled using a subcutaneous dose of 2,7 mg/kg. Also, comparatively studied the antiepileptic activity of triazole derivatives with the well-known antiepileptic drug carbamazepine. In the conducted studies the studied compound showed carbamazepine-like activity at doses of 3 and 10 mg/kg in the model of seizures caused by strychnine, while at a dose of 30 mg/kg it showed high activity and in models induced using bicuculin and isoniazid, the studied drug showed activity similar to carbamazepine. On the contrary, the model of seizures induced by PTZ showed high activity at doses of 3, 10 and 30 mg/kg. The results obtained showed that triazole derivative had a pronounced antiepileptic activity, and further study can be proposed as a potential antiepileptic drug.
Keywords: Benzodiazepines; Carbamazepine; Epilepsy; Pentylenetetrazole; Seizures; Sodium Channels Back to TOC