Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).
Efforts to improve the properties of the well studied ketooxazole FAAH inhibitor OL-135 resulted in the discovery of a novel propylpiperidine series of FAAH inhibitors that has a modular design and superior properties to OL-135. The efficacy of one of these compounds was demonstrated in a rat spinal nerve ligation model of neuropathic pain in rats.
Timmons
Amy
A
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Seierstad
Mark
M
Apodaca
Rich
R
Epperson
Matt
M
Pippel
Dan
D
Brown
Sean
S
Chang
Leon
L
Scott
Brian
B
Webb
Michael
M
Chaplan
Sandra R
SR
Breitenbucher
J Guy
JG
D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D001665:Binding Sites; D006801:Humans; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010146:Pain / Q000188:drug therapy* / Q000201:enzymology*; D010147:Pain Measurement / Q000187:drug effects*; D011725:Pyridines / Q000494:pharmacology; D051381:Rats; D013127:Spinal Nerves / Q000187:drug effects* / Q000293:injuries; D013329:Structure-Activity Relationship; D000099252:Fatty Acid Amide Hydrolases
D000581:Amidohydrolases; D010080:Oxazoles; D011725:Pyridines; D000099252:Fatty Acid Amide Hydrolases; C495479:1-oxo-1-(5-(2-pyridyl)-2-yl)-7-phenylheptane