Publications by authors named "Jennifer E Cryan"

1 Publications

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Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.

Bioorg Med Chem Lett 2008 Oct 31;18(20):5609-13. Epub 2008 Aug 31.

Neurology CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.

6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.
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October 2008