DESIGN OF NOVEL AGENTS FOR THE THERAPY OF NON-INSULIN-DEPENDENT DIABETES-MELLITUS (NIDDM)

Authors
BELL P CHEON SH FILLERS S FOLEY J FRASER J SMITH H YOUNG D REVESZ L
Citation
P. Bell et al., DESIGN OF NOVEL AGENTS FOR THE THERAPY OF NON-INSULIN-DEPENDENT DIABETES-MELLITUS (NIDDM), Bioorganic & medicinal chemistry letters, 3(6), 1993, pp. 1007-1012
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
6
Year of publication
1993
Pages
1007 - 1012
Database
ISI
SICI code
0960-894X(1993)3:6<1007:DONAFT>2.0.ZU;2-Y
Abstract
Methylenecyclopropylacetate 1 - the hypoglycemic but toxic metabolite of hypoglycin A (2) - was chosen as a lead structure for the design of novel agents to treat NIDDM. The successful retargeting of 1 from sho rt- and medium-chain acyl CoA beta-dehydrogenase inhibition towards th e selective blockade of long-chain beta - dehydrogenase yielded the no vel hypoglycemic compound 3d1, devoid of toxic aciduria associated wit h 1 itself.