Jw. Ellingboe et al., ANTIHYPERGLYCEMIC ACTIVITY OF NOVEL NAPHTHALENYL 3H-1,2,3,5-OXATHIADIAZOLE 2-OXIDES, Journal of medicinal chemistry, 36(17), 1993, pp. 2485-2493
A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepar
ed and tested for antihyperglycemic activity in the db/db mouse, a mod
el for type 2 (non-insulin dependent) diabetes mellitus. Substitution
at the 1-, 5-, or 8-positions of the naphthalene ring with a halogen w
as found to be beneficial to antihyperglycemic activity. onaphthalen-2
-yl)methyl]-3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most po
tent compounds in this series, was selected for further pharmacologica
l evaluation.