Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.

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Henry JR, Li Y, Warshawsky AM, Brozinick JT, Hawkins ED, Misener EA, Briere DA, Montrose-Rafizadeh C, Zink RW, Yumibe NP, Ajamie RT, Wilken B, Devanarayan V

Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6293-7. Epub 2006 Sep 26.

PubMed ID
17005393 [ View in PubMed
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Abstract

Novel tetrahydroisoquinolines have been developed as potent PPAR ligands. Evaluation of these compounds in PPARgamma responsive models of type 2 diabetes is described.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaIC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)657N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaIC 50 (nM)48N/AN/ADetails
TroglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)2235N/AN/ADetails
TroglitazonePeroxisome proliferator-activated receptor gammaIC 50 (nM)1285N/AN/ADetails