N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1).
High throughput screening of our compound library revealed a series of N-pyridyl-3-benzamides as low micromolar agonists of the human TRPV1 receptor. Synthesis of analogs in this series led to the discovery of a series of N-quinolin-3-yl-benzamides as low nanomolar antagonists of human TRPV1.
Jetter
Michele C
MC
Johnson & Johnson Pharmaceutical Research and Development, Research and Early Development, Welsh and McKean Roads, Spring House, PA 19477, USA. michele137@comcast.net
McNally
James J
JJ
Youngman
Mark A
MA
McDonnell
Mark E
ME
Dubin
Adrienne E
AE
Nasser
Nadia
N
Zhang
Sui-Po
SP
Codd
Ellen E
EE
Colburn
Ray W
RW
Stone
Dennis R
DR
Brandt
Michael R
MR
Flores
Christopher M
CM
Dax
Scott L
SL
D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D003432:Cross-Linking Reagents / Q000737:chemistry; D006801:Humans; D006930:Hyperalgesia / Q000188:drug therapy; D007546:Isoquinolines / Q000737:chemistry*; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000037:antagonists & inhibitors* / Q000378:metabolism*
D001549:Benzamides; D003432:Cross-Linking Reagents; D007546:Isoquinolines; D011725:Pyridines; D050916:TRPV Cation Channels; C494484:TRPV1 receptor; C023666:pyridine