A new class of histamine H 3-Receptor antagonists: synthesis and structure–Activity relationships of 7, 8, 9, 10-Tetrahydro-6H-cyclohepta [b] quinolines

…, TA Esbenshade, YL Bennani, AA Hancock

Index: Turner, Sean C.; Esbenshade, Timothy A.; Bennani, Youssef L.; Hancock, Arthur A. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 13 p. 2131 - 2135

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Citation Number: 25

Abstract

The synthesis and biological evaluation of novel cycloheptaquinoline antagonists of the human H3 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 H3 receptor ...