Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
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.
Zhao
Hongyu
H
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
Serby
Michael D
MD
Smith
Harriet T
HT
Cao
Ning
N
Suhar
Tom S
TS
Surowy
Teresa K
TK
Camp
Heidi S
HS
Collins
Christine A
CA
Sham
Hing L
HL
Liu
Gang
G
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D005021:Ethylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013230:Stearoyl-CoA Desaturase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D004791:Enzyme Inhibitors; D005021:Ethylamines; D010880:Piperidines; D013230:Stearoyl-CoA Desaturase