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  • Title: Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.
    Author: Bergmeier SC, Ismail KA, Arason KM, McKay S, Bryant DL, McKay DB.
    Journal: Bioorg Med Chem Lett; 2004 Jul 16; 14(14):3739-42. PubMed ID: 15203153.
    Abstract:
    The development of novel agents for the differentiation of neuronal nicotinic acetylcholine receptors (nAChRs) is important for the treatment of a variety of pathological conditions. We have prepared and evaluated a number of simpler analogues of the norditerpeniod alkaloid methyllycaconitine (MLA) in an effort to understand molecular determinants of nAChR*small molecule interactions. We have previously reported the synthesis and evaluation of a series of ring E analogues of MLA. We report here the optimization of the alpha3beta4* functional activity of this series of compounds through modification of the ester.
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