期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 17, 页码 4533-4536出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.06.026
关键词
TRPV1 antagonist; VR1 antagonist; vanilloid
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. (c) 2006 Elsevier Ltd. All rights reserved.
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