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

被引:15
|
作者
BELL, P [1 ]
CHEON, SH [1 ]
FILLERS, S [1 ]
FOLEY, J [1 ]
FRASER, J [1 ]
SMITH, H [1 ]
YOUNG, D [1 ]
REVESZ, L [1 ]
机构
[1] SANDOZ LTD,RES INST,CH-4002 BASEL,SWITZERLAND
关键词
D O I
10.1016/S0960-894X(00)80277-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 short- and medium-chain acyl CoA beta-dehydrogenase inhibition towards the selective blockade of long-chain beta - dehydrogenase yielded the novel hypoglycemic compound 3d1, devoid of toxic aciduria associated with 1 itself.
引用
收藏
页码:1007 / 1012
页数:6
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