A series of 2-oxiranecarboxylate derivatives were prepared as carnitine pal
mitoyl transferase I (CPT-I) inhibitors for the development of new antidiab
etic agents. The syntheses and biological activities were reported. The mos
t promising derivative (13b) showed 2.5 times more hypoglycemic activity an
d 2 times lower acute toxicity compared to Etomoxir ((3)).