In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase

Derek B Lowe; Steven Magnuson; Ning Qi; Ann-Marie Campbell; James Cook; Zhenqiu Hong; Ming Wang; Mareli Rodriguez; Furahi Achebe; Harold Kluender; Wai C Wong; William H Bullock; Arthur I Salhanick; Terri Witman-Jones; Mary E Bowling; Christine Keiper; Kevin B Clairmont

doi:10.1016/j.bmcl.2004.04.015

In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3155-9. doi: 10.1016/j.bmcl.2004.04.015.

Authors

Derek B Lowe¹, Steven Magnuson, Ning Qi, Ann-Marie Campbell, James Cook, Zhenqiu Hong, Ming Wang, Mareli Rodriguez, Furahi Achebe, Harold Kluender, Wai C Wong, William H Bullock, Arthur I Salhanick, Terri Witman-Jones, Mary E Bowling, Christine Keiper, Kevin B Clairmont

Affiliation

¹ Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. derek.lowe.b@bayer.com

PMID: 15149665
DOI: 10.1016/j.bmcl.2004.04.015

Abstract

A series of (5-(2H)-isoxazolonyl) ureas were developed as nanomolar inhibitors of hormone-sensitive lipase, an enzyme of potential importance in the treatment of diabetes.

MeSH terms

Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Hypoglycemic Agents / chemistry*
Hypoglycemic Agents / pharmacology
Isoxazoles / chemistry*
Isoxazoles / pharmacology
Sterol Esterase / antagonists & inhibitors*
Sterol Esterase / metabolism
Structure-Activity Relationship
Urea / chemistry*
Urea / pharmacology

Substances

Enzyme Inhibitors
Hypoglycemic Agents
Isoxazoles
Urea
Sterol Esterase