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Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Apr 01; Vol. 19 (7), pp. 2048-52. Date of Electronic Publication: 2009 Feb 08. - Publication Year :
- 2009
-
Abstract
- We identified a series of structurally novel SCD (Delta9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modification of the central bicyclic scaffold has proven key to our potency optimization effort. The most potent analog (8g) had IC(50) value of 50 pM in a HEPG2 SCD assay and has been shown to be metabolically stable and selective against Delta5 and Delta6 desaturases.
- Subjects :
- Animals
Cell Line
Drug Evaluation, Preclinical
Enzyme Inhibitors metabolism
Enzyme Inhibitors pharmacology
Humans
Inhibitory Concentration 50
Microsomes metabolism
Pteridines metabolism
Pteridines pharmacology
Quinoxalines pharmacology
Rats
Stearoyl-CoA Desaturase metabolism
Structure-Activity Relationship
Enzyme Inhibitors chemistry
Pteridines chemistry
Quinoxalines chemistry
Stearoyl-CoA Desaturase antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19249203
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.02.019