Synthesis of 2-Amino-5-sulfanyl-1,3,4-thiadiazole Derivatives as Anticonvulsant Agents
سال انتشار: 1398
نوع سند: مقاله کنفرانسی
زبان: انگلیسی
مشاهده: 416
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شناسه ملی سند علمی:
SRMMED22_403
تاریخ نمایه سازی: 19 آبان 1398
چکیده مقاله:
Background:1,3,4-thiadiazoles are associated with diverse biocidal activities. A large number of 1,3,4-thiadiazoles have been reported as anticancer, antitubercular, antiflammatory, and pesticide agents. This compounds possessed potent anticonvulsant activity in wide range preclinical in vitro and in vivo models. Material and methods: The study is devoted to the design and synthesis of new 2,5-disubstituted 1,3,4-thiadiazoles 3a-d as a promising muilt-targeting pharmacological scaffold. Heterocyclization of thiosemicarbazide 1 with carbon disulfide lead to the intermediate 5-amino-1,3,4-thiadiazole-2-thiole 2. Further S-alkylation of compound 2 with halo-acetophenone allowed to abtain the target 2-((5-amino-1,3,4-thiadiazol-2-yl) thio)-1-phenylethan-1-one derivatives 3a-d. The reduction of compounds with sodium borohydride was studied and resulted in 4a-d compounds. Results: The structures of these compounds were stablished by means of 1HNMR. Conclusions: The SAR study of synthesized compounds reveals that halo-acetophenone attached to 1,3,4-thiadiazole ring as substituent linked to sulfonyl group could be studied for anticonvulsant efficacy. Additionally, anticonvulsant activity of carbonyl compounds could be compared to hydroxyl-containing structures.
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نویسندگان
Elham Amjadi
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
Elmira Nazer
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
Hamideh Ahadi
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
Saeed Emami
Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran