Dibasic non-imidazole histamine H 3 receptor antagonists with a rigid biphenyl scaffold

…, L Flammini, S Bertoni, V Ballabeni, E Barocelli…

Index: Morini, Giovanni; Comini, Mara; Rivara, Mirko; Rivara, Silvia; Lorenzi, Simone; Bordi, Fabrizio; Mor, Marco; Flammini, Lisa; Bertoni, Simona; Ballabeni, Vigilio; Barocelli, Elisabetta; Plazzi, Pier Vincenzo Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 15 p. 4063 - 4067

Full Text: HTML

Citation Number: 22

Abstract

A class of rigid, dibasic, non-imidazole H3 antagonists was developed, starting from a series of previously described flexible compounds. The original polymethylene chain between two tertiary amine groups was replaced by a rigid scaffold, composed by a phenyl ring or a biphenyl fragment. Modulation of the distance between the two amine groups, and of their alkyl substituents, was driven by superposition of molecular models and docking into a ...