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

Lee, J; Park, S U; Kim, J Y; Kim, J K; Lee, J; Oh, U; Marquez, V E; Beheshti, M; Wang, Q J; Modarres, S; Blumberg, P M

Lee, J; Park, S U; Kim, J Y; Kim, J K; Lee, J; Oh, U; Marquez, V E; Beheshti, M; Wang, Q J; Modarres, S; Blumberg, P M.

Affiliation

Lee J; Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Korea.

Bioorg Med Chem Lett ; 9(20): 2909-14, 1999 Oct 18.

Article in En | MEDLINE | ID: mdl-10571146

ABSTRACT

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.

Subject(s)

Amides/chemistry; Esters/chemistry; Homovanillic Acid/analogs & derivatives; Receptors, Drug/agonists; Drug Design; Homovanillic Acid/chemical synthesis; Homovanillic Acid/pharmacology

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Collection: 01-internacional Database: MEDLINE Main subject: Receptors, Drug / Esters / Amides / Homovanillic Acid Language: En Journal: Bioorg Med Chem Lett Year: 1999 Document type: Article

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