Dibasic non-imidazole histamine H3 receptor antagonists with a rigid biphenyl scaffold
| Autor: | Marco Mor, Mara Comini, Lisa Flammini, Simona Bertoni, Vigilio Ballabeni, Simone Lorenzi, Silvia Rivara, Mirko Rivara, Giovanni Morini, Fabrizio Bordi, Pier Vincenzo Plazzi, Elisabetta Barocelli |
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| Rok vydání: | 2006 |
| Předmět: |
Models
Molecular Molecular model Tertiary amine Stereochemistry Clinical Biochemistry Guinea Pigs Histamine Antagonists Pharmaceutical Science Biochemistry Cell Line chemistry.chemical_compound Histamine receptor Drug Discovery Imidazole Animals Humans Receptors Histamine H3 Molecular Biology Dibasic acid Organic Chemistry Imidazoles Rats chemistry Docking (molecular) Molecular Medicine Amine gas treating Histamine H3 receptor |
| Zdroj: | Bioorganicmedicinal chemistry letters. 16(15) |
| ISSN: | 0960-894X |
| Popis: | A class of rigid, dibasic, non-imidazole H 3 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 receptor model, resulting in the identification of 1,1′-[biphenyl-4,4′-diylbis(methylene)]bis-piperidine ( 5 ) as a subtype-selective H 3 antagonist with high binding affinity (p K i = 9.47) at human H 3 histamine receptor. |
| Databáze: | OpenAIRE |
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