Novel H3 receptor antagonists. Sulfonamide homologs of histamine
Autor: | Adriano Afonso, Shirley M. Willams, John A. Hey, Hoyan She, Michael Connolly, Maria A. Rivelli, Ronald L. Wolin, Robert E. West |
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Rok vydání: | 1998 |
Předmět: |
Stereochemistry
Guinea Pigs Clinical Biochemistry Histamine Antagonists Pharmaceutical Science Ring (chemistry) Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Piperidines Drug Discovery Animals Receptors Histamine H3 Imidazole Molecular Biology chemistry.chemical_classification Sulfonamides Molecular Structure Cell Membrane Organic Chemistry Antagonist Brain In vitro Sulfonamide Kinetics chemistry Drug Design Molecular Medicine Histamine H3 receptor Histamine |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 8:2157-2162 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(98)00379-5 |
Popis: | Sulfonamides derived from 4(5)-(ω-aminoalkyl)-1H-imidazoles containing chain lengths of three- to five-carbons were synthesized. Good to moderate H3 receptor binding affinities were observed for several butyl and pentyl homologs, whereas binding affinities were considerably weaker in the propyl series. Separation of the imidazole ring and the sulfonamide unit by a four- or five-carbon tether afforded potent H3 receptor antagonists. |
Databáze: | OpenAIRE |
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