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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 32, 2017 - Issue 1
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Research Article

Novel FFA1 (GPR40) agonists containing spirocyclic periphery: polar azine periphery as a driver of potency

Mikhail KrasavinSaint Petersburg State University, Saint Petersburg, Russian Federation; Correspondence[email protected]
,
Alexey LukinLomonosov Institute of Fine Chemical Technologies, Moscow Technological University, Moscow, Russian Federation;
,
Daria BagnyukovaLomonosov Institute of Fine Chemical Technologies, Moscow Technological University, Moscow, Russian Federation;
,
Nikolay ZhuriloLomonosov Institute of Fine Chemical Technologies, Moscow Technological University, Moscow, Russian Federation;
,
Ihor ZahanichEnamine Ltd., Kyiv, Ukraine;
&
Sergey ZozulyaEnamine Ltd., Kyiv, Ukraine; ;Taras Shevchenko National University, Kyiv, Ukraine
Pages 29-36 | Received 22 Jul 2016, Accepted 20 Aug 2016, Published online: 26 Oct 2016

References

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  • Krasavin M, Lukin A, Zhurilo N, et al. Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold. Bioorg Med Chem 2016;24:2954–63.
  • Lukin A, Bagnyukova D, Zhurilo N, Krasavin M. Gram-scale synthesis of a novel core building block for the new GPR40 agonist design. Lett Org Chem. 2016. [Epub ahead of print]. doi: 10.2174/1570178613666160805115331.
  • Lukin A, Bagnyukova D, Kalichenkova N, et al. Spirocyclic amino alcohol building blocks prepared via a Prins-type cyclization in aqueous sulfuric acid. Tetrahedron Lett 2016;57:3311–14.
  • Krasavin M, Lukin A, Bagnyukova D, et al. Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835. Bioorg Med Chem. 2016. [Epub ahead of print]. doi: 10.1016/j.bmc.2016.09.004.
  • Negoro N, Sasaki S, Mikami S, et al. Discovery of TAK-875: a potent, selective, and orally bioavailable GPR40 agonist. ACS Med Chem Lett 2010;1:290–4.
  • Ichimura A, Hirasawa A, Hara T, Tsujimoto G. Free fatty acid receptors act as nutrient sensors to regulate energy homeostasis. Prostaglandins Other Lipid Mediat 2009;89:82–8.
  • Calculated using Molinspiration Online Property Calculator. Available from: www.molinspiration.com [last accessed 20 July 2016].

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