Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors. 2007

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

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.

UI MeSH Term Description Entries
D010880 Piperidines A family of hexahydropyridines.
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D005021 Ethylamines Derivatives of ethylamine (the structural formula CH3CH2NH2).
D013230 Stearoyl-CoA Desaturase An enzyme that catalyzes the formation of oleoyl-CoA, A, and water from stearoyl-CoA, AH2, and oxygen where AH2 is an unspecified hydrogen donor. Stearyl-CoA Desaturase,Stearate Desaturase,delta-9 Desaturase,Desaturase, Stearate,Desaturase, Stearoyl-CoA,Desaturase, Stearyl-CoA,Desaturase, delta-9,Stearoyl CoA Desaturase,Stearyl CoA Desaturase,delta 9 Desaturase
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013379 Substrate Specificity A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts. Specificities, Substrate,Specificity, Substrate,Substrate Specificities

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