Journal of Medicinal Chemistry p. 2280 - 2284 (1986)
Update date:2022-08-04
Topics:
Stillings, Michael R.
Welbourn, Anthony P.
Walter, Donald S.
This paper describes the synthesis and pharmacological evaluation of a number of substituted 1,3,4-thiadiazoles.The first member of the series, 2-(aminomethyl)-5-(2-biphenylyl)-1,3,4-thiadiazole (7) was found to possess potent anticonvulsant properties in rats and mice and compared favorably with the standard anticonvulsant drugs phenytoin, phenobarbital, and carbamazepine in a number of test situations.The potency of compound 7 was maintained on alkylation of the side-chain nitrogen atom; however, aryl substitution or chain lengthening caused a drop in potency.Replacement of the 2-biphenylyl group by phenyl or benzyl also lead to inactive compounds.
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