Title of article
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1
Author/Authors
Susan M. Westaway، نويسنده , , Mervyn Thompson، نويسنده , , Harshad K. Rami، نويسنده , , Geoffrey Stemp، نويسنده , , Leontine S. Trouw، نويسنده , , Darren J. Mitchell، نويسنده , , Jon T. Seal، نويسنده , , Stephen J. Medhurst، نويسنده , , Sarah C. Lappin، نويسنده , , James Biggs، نويسنده , , James Wright، نويسنده , , Sandra Arpino، نويسنده , , Jeffrey C. Jerman، نويسنده , , Jennifer E. Cryan، نويسنده , , Vicky Holland، نويسنده , , Kim Y. Winborn، نويسنده , , Tanya Coleman، نويسنده , , Alexander J. Stevens، نويسنده , , John B. Davis، نويسنده , , Martin J. Gunthorpe، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
5609
To page
5613
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.
Keywords
SB-782443 , Vanilloid , TRPV1 antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800069
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