Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha 7 selectivity

G Karig, J M Large, C G V Sharples, A Sutherland, T Gallagher, S Wonnacott

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

Four racemic phenyl-substituted analogues 3-6 of the potent nicotinic agonist UB-165 1 have been synthesised and evaluated against the alpha(4)beta(2), alpha(3)beta(4), and alpha(7) neuronal nicotinic receptors. The 2'-phenyl derivative 3 shows no activity at these major receptor subtypes. while the 4'-phenyl analogue 4 shows an enhanced level Of a7 selectivity as compared to UB-165 and deschloro UB-165 2. These results are discussed within the context of recent pharmacophore models.
Original languageEnglish
Pages (from-to)2825-2828
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume13
Issue number17
DOIs
Publication statusPublished - 1 Sep 2003

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