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A new class of histamine H3-Receptor antagonists: synthesis and structure–Activity relationships of 7,8,9,10-Tetrahydro-6H-cyclohepta[b]quinolines
- Source :
- Bioorganic & Medicinal Chemistry Letters. 13:2131-2135
- Publication Year :
- 2003
- Publisher :
- Elsevier BV, 2003.
-
Abstract
- The synthesis and biological evaluation of novel cycloheptaquinoline antagonists of the human H(3) receptor are described. Two series of compounds, bearing either an amino substituent or an alkyne linker at the 11-position, were investigated. Modifications of the amino substituents, optimization of chain length and the effect of conformational restraints are described. Several compounds with high affinity and selectivity for the H(3) receptor were discovered.
- Subjects :
- Magnetic Resonance Spectroscopy
Tertiary amine
Stereochemistry
Clinical Biochemistry
Drug Evaluation, Preclinical
Histamine Antagonists
Molecular Conformation
Substituent
Pharmaceutical Science
Alkyne
Biochemistry
Chemical synthesis
Mass Spectrometry
Structure-Activity Relationship
chemistry.chemical_compound
Diamine
Drug Discovery
Animals
Humans
Receptors, Histamine H3
Structure–activity relationship
Receptors, Histamine H2
Receptors, Histamine H1
Cloning, Molecular
Receptor
Molecular Biology
Cerebral Cortex
chemistry.chemical_classification
Organic Chemistry
General Medicine
Recombinant Proteins
Rats
Chain length
chemistry
Quinolines
Molecular Medicine
Indicators and Reagents
Histamine H3 receptor
Selectivity
Linker
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....60a267decde333cbcc2e51fc5452fbae
- Full Text :
- https://doi.org/10.1016/s0960-894x(03)00356-1