A new class of histamine H(3)-receptor antagonists: synthesis and structure-activity relationships of 7,8,9,10-tetrahydro-6H-cyclohepta[b]quinolines.

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.

journal_name

Bioorg Med Chem Lett

authors

Turner SC,Esbenshade TA,Bennani YL,Hancock AA

doi

10.1016/s0960-894x(03)00356-1

subject

Has Abstract

pub_date

2003-07-07 00:00:00

pages

2131-5

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960894X03003561

journal_volume

13

pub_type

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