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Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Jan 15; Vol. 20 (2), pp. 499-502. Date of Electronic Publication: 2009 Nov 26. - Publication Year :
- 2010
-
Abstract
- A series of stearoyl-CoA desaturase 1 (SCD1) inhibitors were developed. Investigations of enzyme potency and metabolism led to the identification of the thiadiazole-pyridazine derivative MF-438 as a potent SCD1 inhibitor. MF-438 exhibits good pharmacokinetics and metabolic stability, thereby serving as a valuable tool for further understanding the role of SCD inhibition in biological and pharmacological models of diseases related to metabolic disorders.<br /> (Copyright 2009 Elsevier Ltd. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacokinetics
Mice
Microsomes, Liver metabolism
Pyridazines chemistry
Pyridazines pharmacokinetics
Rats
Stearoyl-CoA Desaturase metabolism
Structure-Activity Relationship
Thiadiazoles chemistry
Thiadiazoles pharmacokinetics
Enzyme Inhibitors chemical synthesis
Pyridazines chemical synthesis
Stearoyl-CoA Desaturase antagonists & inhibitors
Thiadiazoles chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20004097
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.11.111