STUDIES ON CEREBRAL PROTECTIVE AGENTS .10. SYNTHESIS AND EVALUATION OF ANTICONVULSANT ACTIVITIES FOR NOVEL 4,5,6,7-TETRAHYDROTHIENO[3,2-C]PYRIDINES AND RELATED-COMPOUNDS

Novel 4,5,6,7-tetrahydrothieno[3,2-c]pyridines, 1-thienyl-1,2,3,4-tetr ahydroisoquinolines and related compounds, in which the benzene rings of(+)- 1 (FR115427) were replaced with heteroaromatic rings such as th iophene, furan, benzothiophene and indole, were synthesized and evalua ted for anticonvulsant activity against i.c.v. N-methyl-D-aspartate (N MDA)-induced seizures in mice. Among these compounds, l-4-phenyl-4,5,6 ,7-tetrahydrothieno[3,2-c]pyridine hydrochloride ((+)-2a), thyl-4-(2-t hienyl)-1,5,6,7-tetrahydrothieno[3,2-c] pyridine hydrochloride ((+)-2g ), and -methyl-1-(2-thienyl)-1,2,3,4-tetrahydrisquinoline hydrochlorid e ((-)-3a) showed significant anticonvulsant activity, The structure-a ctivity relationships with regard to the anticonvulsant activity of th is series of compounds are discussed.