N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1

…, HK Rami, G Stemp, AJ Stevens, M Thompson…

Index: Westaway, Susan M.; Chung, Ying-Kit; Davis, John B.; Holland, Vicky; Jerman, Jeffrey C.; Medhurst, Stephen J.; Rami, Harshad K.; Stemp, Geoffrey; Stevens, Alexander J.; Thompson, Mervyn; Winborn, Kim Y.; Wright, James Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 17 p. 4533 - 4536

Full Text: HTML

Citation Number: 35

Abstract

Starting from the high throughput screening hit (3), novel N-tetrahydroquinolinyl, N- quinolinyl and N-isoquinolinyl carboxamides have been identified as potent antagonists of the ion channel TRPV1. The N-quinolinylnicotinamide (46) showed excellent potency at human, guinea pig and rat TRPV1, a favourable in vitro DMPK profile and activity in an in vivo model of inflammatory pain.