Back to Search
Start Over
FXR agonist activity of conformationally constrained analogs of GW 4064.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Aug 15; Vol. 19 (16), pp. 4733-9. Date of Electronic Publication: 2009 Jun 21. - Publication Year :
- 2009
-
Abstract
- Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.
- Subjects :
- Animals
Binding Sites
Computer Simulation
Crystallography, X-Ray
Humans
Isoxazoles pharmacology
Naphthalenes pharmacokinetics
Rats
Receptors, Cytoplasmic and Nuclear metabolism
Structure-Activity Relationship
Thiophenes pharmacokinetics
Isoxazoles chemistry
Naphthalenes chemistry
Receptors, Cytoplasmic and Nuclear agonists
Thiophenes chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19586769
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.06.062