3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists

…, JK Kim, J Lee, U Oh, VE Marquez, M Beheshti…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 20 p. 2909 - 2914

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Citation Number: 19

Abstract

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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