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Discovery of a New Class of Non‐imidazole Oxazoline‐Based Histamine H3 Receptor (H3R) Inverse Agonists
Authors:Sylvain Célanire Dr  Maikel Wijtmans Dr  Bernard Christophe Dr  Philippe Collart  Iwan de?Esch Dr  Donald Dassesse Dr  Christel Delaunoy  Frédéric Denonne Dr  Véronique Durieu  Edith Gelens Dr  Michel Gillard Dr  Bénédicte Lallemand  Yves Lamberty Dr  Florence Lebon Dr  Jean‐Marie Nicolas Dr  Luc Quéré Dr  Erwin Snip Dr  Alain Vanbellinghen  Nathalie Van?houtvin  Valérie Verbois  Henk Timmerman Prof?Dr  Patrice Talaga Dr  Rob Leurs Prof?Dr  Laurent Provins Dr
Affiliation:1. UCB New Medicines, Chemin du Foriest, 1420 Braine‐L'Alleud (Belgium), Fax: (+32)?2‐3863669;2. Present address: Addex Pharma, Geneva (Switzerland);3. Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Faculty of Exact Sciences, VU University of Amsterdam, Amsterdam (The Netherlands)
Abstract:H 3 R inverse agonists based on an aminopropoxy‐phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.
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Keywords:cognitive disorders  druglike properties  histamine H3 receptors  structure–  activity relationships  oxazolines
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