Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines.
The synthesis and anticonvulsant activity of a number of 2-aryl-5-guanidino-1,3,4 thiadiazoles are described. The unsubstituted guanidine 2a was found to possess potent anticonvulsant properties; considerable reduction or loss of activity however was observed with the majority of the substituted guanidines. Incorporation of the guanidine group into an imidazoline ring also resulted in a loss of activity. Secondary pharmacological evaluation confirmed the anticonvulsant properties of 2a but also revealed that the compound exhibited a considerable degree of sedative activity.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004597:Electroshock; D006146:Guanidines / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity; D051379:Mice; D010433:Pentylenetetrazole; D051381:Rats; D012640:Seizures / Q000188:drug therapy* / Q000209:etiology; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity
D006146:Guanidines; D013830:Thiadiazoles; D010433:Pentylenetetrazole