Christiansen, E. et al. (2012) Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. Journal of Medicinal Chemistry, 55(14), pp. 6624-6628. (doi: 10.1021/jm3002026)
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Abstract
FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Hudson, Dr Brian and Milligan, Professor Graeme |
| Authors: | Christiansen, E., Due-Hansen, M.E., Urban, C., Grundmann, M., Schröder, R., Hudson, B.D., Milligan, G., Cawthorne, M.A., Kostenis, E., Kassack, M.U., and Ulven, T. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Molecular Biosciences |
| Journal Name: | Journal of Medicinal Chemistry |
| ISSN: | 0022-2623 |
| Published Online: | 25 June 2012 |
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