Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.
We report on a series of alpha-substituted-beta-tetralin-derived and related phenethyl-based isoquinolinyl and hydroxynaphthyl ureas as potent antagonists of the human TRPV1 receptor. The synthesis and Structure-activity relationships (SAR) of the series are described.
Jetter
Michele C
MC
Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA. mjetter@prdus.jnj.com
Youngman
Mark A
MA
McNally
James J
JJ
McDonnell
Mark E
ME
Zhang
Sui-Po
SP
Dubin
Adrienne E
AE
Nasser
Nadia
N
Codd
Ellen E
EE
Flores
Christopher M
CM
Dax
Scott L
SL
D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
D050916:TRPV Cation Channels; C494482:TRPV1 protein, human; D013764:Tetrahydronaphthalenes; D014508:Urea