Title compds. [I; Y = Q1-Q3; R = H, Me; R1 = H, halo, OH, alkyl, alkenyl, alkoxy, alkylamino, (substituted) Ph, naphthyl, PhO, naphthyloxy, PhNH; n = 0, 1; X = (substituted) Ph, pyridyl, naphthyl, quinolyl, isoquinolyl; with specific exceptions], were prepd. Thus, (2E)-N-(isoquinolin-5-yl)-3-(2,6,6-trimethyl-3-phenoxycyclohex-1-enyl)acrylamide (3-step prepn. given) showed a Ki value of 4.93 nM in competition binding expts. with [3H]-RTX to TRPV1 expressed in rat spinal cord.
Preparation of isoquinolinyl cyclohexenylacrylamides as transient receptor potential vanilloid 1 (TRPV1) receptor antagonists
BARALDI, Pier Giovanni;BOREA, Pier Andrea;PAVANI, Maria Giovanna;FRUTTAROLO, Francesca;TREVISANI, Marcello
2008
Abstract
Title compds. [I; Y = Q1-Q3; R = H, Me; R1 = H, halo, OH, alkyl, alkenyl, alkoxy, alkylamino, (substituted) Ph, naphthyl, PhO, naphthyloxy, PhNH; n = 0, 1; X = (substituted) Ph, pyridyl, naphthyl, quinolyl, isoquinolyl; with specific exceptions], were prepd. Thus, (2E)-N-(isoquinolin-5-yl)-3-(2,6,6-trimethyl-3-phenoxycyclohex-1-enyl)acrylamide (3-step prepn. given) showed a Ki value of 4.93 nM in competition binding expts. with [3H]-RTX to TRPV1 expressed in rat spinal cord.File in questo prodotto:
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