Bioorganic and Medicinal Chemistry Letters p. 2909 - 2914 (1999)
Update date:2022-08-05
Topics: Pharmacological evaluation Esterification In vitro Testing In Vivo Testing Structure-Activity Relationship (SAR) Biological assay Agonist Synthetic derivatives
Lee, Jeewoo
Park, Shin-Ung
Kim, Ji-Young
Kim, Jin-Kwan
Lee, Jiyoun
Oh, Uhtaek
Marquez, Victor E.
Beheshti, Maryam
Wang, Qiming J.
Modarres, Shayan
Blumberg, Peter M.
A series of 3-acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid were designed and synthesized as vanilloid receptor agonists containing the three principal pharmacophores of resiniferatoxin. Amide analogues 23, 5 and 11 were found to be potent agonists in vanilloid receptor assay both for ligand binding and for activation.
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