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

DOI: 10.1016/S0960-894X(99)00513-2

Source and publish data:

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

Authors:

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.

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Article abstract of DOI:10.1016/S0960-894X(99)00513-2

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.

Full text of DOI:10.1016/S0960-894X(99)00513-2

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