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Paper | Special issue | Vol 52, No. 3, 2000, pp.1087-1103
Published online, 1st January, 1970
DOI: 10.3987/COM-98-8235
Design and Syntheses of 2-Oxiranecarboxylate Derivatives and Their Hypoglycemic Activities

Sang-sup Jew,* Eun-kyung Kim, Sun-mi Je, Long-Xuan Zhao, Hyung-ook Kim, Hyeung-geun Park, Kwang-ho Ko, Won-ki Kim, Hwa-Jung Kim, Jae Hoon Cheong, and Eung-Seok Lee*

*College of Pharmacy, Seoul National University, Shillim-Dong, San 56-1, Kwanak-Gu, Seoul 151-741, Korea

Abstract

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