A new class of histamine H 3 receptor antagonists derived from ligand based design

O Roche, RMR Sarmiento

Index: Roche, Olivier; Rodriguez Sarmiento, Rosa Maria Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3670 - 3675

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Citation Number: 41

Abstract

Design and synthesis of highly potent and selective non-imidazole inverse agonists for the histamine H3 receptor is described. The study validates a new pharmacophore model based on the merging of two previously described models. It also demonstrates that the removal of the basic center potentially interacting with ASP3. 32 and common to both models leads to loss of activity, whereas the replacement of the second basic center by an acceptor retains ...