Title compds. [I; wherein X = halo, alkyl, alkoxy, (hetero)aryl; R1 = 2-hydroxyethyl, 2,3-dihydroxypropyl, etc.; R2 = CF3 or t-Bu; R3 and R4 independently = H, CN, alkyl, etc.; including all possible optical isomers and diastereoisomers thereof] were prepd. as TRPV1 (transient receptor potential vanilloid 1) receptor antagonists, useful in the treatment of, e.g., inflammation. Thus, the invention compd. II was prepd. and gave a Ki value of 60 nM in the radioligand binding assay.
Preparation of O-substituted-dibenzyl urea derivatives as TRPV1 receptor antagonists.
BARALDI, Pier Giovanni;BOREA, Pier Andrea;FRUTTAROLO, Francesca;PAVANI, Maria Giovanna;TREVISANI, Marcello
2008
Abstract
Title compds. [I; wherein X = halo, alkyl, alkoxy, (hetero)aryl; R1 = 2-hydroxyethyl, 2,3-dihydroxypropyl, etc.; R2 = CF3 or t-Bu; R3 and R4 independently = H, CN, alkyl, etc.; including all possible optical isomers and diastereoisomers thereof] were prepd. as TRPV1 (transient receptor potential vanilloid 1) receptor antagonists, useful in the treatment of, e.g., inflammation. Thus, the invention compd. II was prepd. and gave a Ki value of 60 nM in the radioligand binding assay.File in questo prodotto:
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