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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

Authors :
Sean C. Turner
Arthur A. Hancock
Youssef L. Bennani
Timothy A. Esbenshade
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.

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