Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors

Hongyu Zhao; Michael D Serby; Harriet T Smith; Ning Cao; Tom S Suhar; Teresa K Surowy; Heidi S Camp; Christine A Collins; Hing L Sham; Gang Liu

doi:10.1016/j.bmcl.2007.03.099

Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3388-91. doi: 10.1016/j.bmcl.2007.03.099. Epub 2007 Apr 5.

Authors

Hongyu Zhao¹, Michael D Serby, Harriet T Smith, Ning Cao, Tom S Suhar, Teresa K Surowy, Heidi S Camp, Christine A Collins, Hing L Sham, Gang Liu

Affiliation

¹ Metabolic Disease Research, Global Pharmaceutical Research and Development, R4MC, AP-10, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. zhao_hongyu@hotmail.com

PMID: 17434733
DOI: 10.1016/j.bmcl.2007.03.099

Abstract

A series of novel stearoyl-CoA desaturase 1 (SCD1) inhibitors were identified by scaffold design based on known SCD1 inhibitors. Large structural changes were made leading to multiple analogs with comparable or improved potency. This approach is valuable for generation of proprietary compounds without conducting a costly high-throughput screening.

MeSH terms

Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology*
Ethylamines / chemical synthesis
Ethylamines / pharmacology*
Piperidines / chemical synthesis
Piperidines / pharmacology*
Stearoyl-CoA Desaturase / antagonists & inhibitors*
Structure-Activity Relationship
Substrate Specificity

Substances

Enzyme Inhibitors
Ethylamines
Piperidines
Stearoyl-CoA Desaturase