Design of α7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies
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- 作者：Aziz Ouacha ; Frederic Pina ; Emilie Bertranda ; Johnny Vercouillieb ; Zuhal Gulhanb ; Cé ; line Mothesc ; Jean-Bernard Deloyec ; Denis Guilloteaub ; Franck Suzeneta ; Sylvie Chalonb ; Sylvain Routiera ; sylvain.routier@univ-orleans.fr" class="auth_mail" title="E-mail the corresponding author
- 关键词：Alpha 7 nicotinic acetylcholine receptors ; Quinuclidine ; Tropane ; Triazole synthesis ; SAR ; In vitro evaluation
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：1 January 2016
- 年：2016
- 卷：107
- 期：Complete
- 页码：153-164
- 全文大小：1791 K
文摘
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30 new potent alpha 7 nAChR ligand synthesized derivatives synthesized.
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2 identified leads exhibited a strong affinity (Ki = 2.3 and 3 nM).
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Leads exhibit strict selectivity toward the α4β2 nicotinic receptor.
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Leads induced a 5HT3 receptors Inhibition with Ki around 3 nM.
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Rational design, synthesis, SAR are depicted.