Diarylacetylene piperidinyl amides as novel anxiolytics.
N-Phenyl-2-[1-[3-(2-pyridinylethynyl)benzoyl]-4-piperidine]acetamide (9) and related piperidine acetamide derivatives have good oral activity in the elevated plus maze, an animal model predictive of clinical efficacy for the treatment of anxiety. Modest affinity was observed for the neurokinin NK-1 and 2 receptors, which are known to be involved in the regulation of mood and emotion.
Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development LLC, Welsh and McKean Roads, Spring House, PA 19477, USA. ckordik@prdus.jnj.com
Cheryl P
CP
Kordik
Chi
C
Luo
Maryann
M
Gutherman
Anil H
AH
Vaidya
Daniel I
DI
Rosenthal
Jeffrey J
JJ
Crooke
Sandra L
SL
McKenney
Carlos R
CR
Plata-Salaman
Allen B
AB
Reitz
D000114:Acetylene / Q000737:chemistry*; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000577:Amides; D014151:Anti-Anxiety Agents; D000114:Acetylene