Phenylacetic acid derivatives as hPPAR agonists.
Article Details
- CitationCopy to clipboard
Santini C, Berger GD, Han W, Mosley R, MacNaul K, Berger J, Doebber T, Wu M, Moller DE, Tolman RL, Sahoo SP
Phenylacetic acid derivatives as hPPAR agonists.
Bioorg Med Chem Lett. 2003 Apr 7;13(7):1277-80.
- PubMed ID
- 12657263 [ View in PubMed]
- Abstract
Beginning with the weakly active lead structure 1, a new series of hPPAR agonists was developed. In vivo glucose and triglyceride lowering activity was obtained by homologation and oxamination to 3, then conversion to substituted benzisoxazoles 4 and 5. Further manipulation afforded benzofurans 6 and 7. Compound 7 was of comparable potency as a glucose and triglyceride lowering agent in insulin resistant rodents to BRL 49653.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rosiglitazone Peroxisome proliferator-activated receptor alpha IC 50 (nM) >5 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor delta IC 50 (nM) >5 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 10 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma IC 50 (nM) 210 N/A N/A Details