Cyclization of thiosemicarbazide derivatives of 5-arylidene-2,4-dioxothiazolidine-3-acetic acids to 1,3,4-thiadiazoles and their pharmacological properties.
By the reaction of (5-arylidene-2,4-dioxothiazolidin-3-yl)acetyl chlorides with 4-phenylthiosemicarbazide, acylthiosemicarbazide derivatives 4-6 were obtained. The cyclization of 4-6 in acid medium led to 1,3,4-thiadiazole derivatives 7-9. The structure of the compounds was confirmed by elemental analysis and IR, H NMR, 13C NMR and MS spectra. The effects of compounds 7 and 9 on the central nervous system (CNS) of mice were studied.
Trotsko
Nazar
N
Department of Organic Chemistry, Medical University, 6 Staszica Str., 20-081 Lublin, Poland. nazartrocko@hotmail.com
Dobosz
Maria
M
Jagiełło-Wójtowicz
Ewa
E
D000085:Acetates; D000700:Analgesics / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002490:Central Nervous System / Q000187:drug effects*; D003500:Cyclization; D004305:Dose-Response Relationship, Drug; D005260:Female; D007274:Injections, Intraperitoneal; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D010146:Pain / Q000188:drug therapy; D010147:Pain Measurement; D012663:Semicarbazides / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013830:Thiadiazoles; D023382:Toxicity Tests, Acute
D000085:Acetates; D000700:Analgesics; D012663:Semicarbazides; D013830:Thiadiazoles