Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.
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Maruyama T, Seki N, Onda K, Suzuki T, Kawazoe S, Hayakawa M, Matsui T, Takasu T, Ohta M
Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.
Bioorg Med Chem. 2009 Aug 1;17(15):5510-9. doi: 10.1016/j.bmc.2009.06.031. Epub 2009 Jun 21.
- PubMed ID
- 19581100 [ View in PubMed]
- Abstract
In the search for potent and selective human beta3-adrenergic receptor (AR) agonists as potential drugs for the treatment of obesity and noninsulin-dependent (type II) diabetes, we prepared a novel series of phenoxypropanolamine derivatives containing the thiourea moiety and evaluated their biological activities at human beta3-, beta2-, and beta1-ARs. Among these compounds, 4-nitrophenylthiourea (18i) and 3-methoxyphenylthiourea (18k) derivatives were found to exhibit potent agonistic activity at the beta3-AR, with EC(50) values of 0.10 and 0.16 microM, respectively, and no agonistic activity for either the beta1- or beta2-AR. In addition, they showed significant hypoglycemic activity in a rodent diabetic model.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Isoprenaline Beta-1 adrenergic receptor EC 50 (nM) 12 N/A N/A Details Isoprenaline Beta-1 adrenergic receptor EC 50 (nM) 1000 N/A N/A Details Isoprenaline Beta-3 adrenergic receptor EC 50 (nM) 100 N/A N/A Details Isoprenaline Beta-3 adrenergic receptor EC 50 (nM) 1000 N/A N/A Details