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Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4ß2α5 nicotinic acetylcholine receptors.
Jin, Zhuang; Khan, Pasha; Shin, Youseung; Wang, Jingyi; Lin, Li; Cameron, Michael D; Lindstrom, Jon M; Kenny, Paul J; Kamenecka, Theodore M.
Afiliação
  • Jin Z; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
  • Khan P; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
  • Shin Y; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
  • Wang J; Department of Neuroscience, University of Pennsylvania, 217 Stemmler Hall, 36th & Hamilton Walk, Philadelphia, PA 19104, USA.
  • Lin L; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
  • Cameron MD; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
  • Lindstrom JM; Department of Neuroscience, University of Pennsylvania, 217 Stemmler Hall, 36th & Hamilton Walk, Philadelphia, PA 19104, USA.
  • Kenny PJ; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
  • Kamenecka TM; Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA. Electronic address: kameneck@scripps.edu.
Bioorg Med Chem Lett ; 24(2): 674-8, 2014 Jan 15.
Article em En | MEDLINE | ID: mdl-24365158
ABSTRACT
The design and synthesis of a series of substituted heteroaromatic α4ß2α5 positive allosteric modulators is reported. The optimization and development of the heteroaromatic series was carried out from NS9283, and several potent analogues, such as 3-(5-(pyridin-3-yl)-2H-tetrazol-2-yl)benzonitrile (5k) and 3,3'-(2H-tetrazole-2,5-diyl)dipyridine (12 h) with good in vitro efficacy were discovered.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores Nicotínicos / Antagonistas Nicotínicos / Agonistas Nicotínicos Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Estados Unidos
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores Nicotínicos / Antagonistas Nicotínicos / Agonistas Nicotínicos Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Estados Unidos