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Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1 |
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| Authors: | Westaway Susan M Thompson Mervyn Rami Harshad K Stemp Geoffrey Trouw Leontine S Mitchell Darren J Seal Jon T Medhurst Stephen J Lappin Sarah C Biggs James Wright James Arpino Sandra Jerman Jeffrey C Cryan Jennifer E Holland Vicky Winborn Kim Y Coleman Tanya Stevens Alexander J Davis John B Gunthorpe Martin J |
| Affiliation: | Neurology CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. sue.m.westaway@gsk.com |
| Abstract: | 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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