Discovery and optimisation of potent and highly subtype selective Nav1.8 inhibitors with reduced cardiovascular liabilities
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we describe the discovery and optimisation of a Nav1.8 inhibiting phenyl imidazole series that delivers chemical equity that possesses high potency and selectivity and...
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| Veröffentlicht in: | MedChemComm 2016-10, Vol.7 (10), p.1925-1931 |
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| creator | Bagal, Sharan K Kemp, Mark I Bungay, Peter J Hay, Tanya L Murata, Yoshihisa Payne, CElizabeth Stevens, Edward B Brown, Alan Blakemore, David C Corbett, Matthew S Miller, Duncan C Omoto, Kiyoyuki Warmus, Joseph S |
| description | Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we describe the discovery and optimisation of a Nav1.8 inhibiting phenyl imidazole series that delivers chemical equity that possesses high potency and selectivity and is capable of demonstrating good oral pharmacokinetics. |
| doi_str_mv | 10.1039/c6md00281a |
| format | Article |
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| ispartof | MedChemComm, 2016-10, Vol.7 (10), p.1925-1931 |
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| language | eng |
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| source | Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection |
| title | Discovery and optimisation of potent and highly subtype selective Nav1.8 inhibitors with reduced cardiovascular liabilities |
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