Bioorganic & Medicinal Chemistry Letters 2003-07-07

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

Sean C Turner, Timothy A Esbenshade, Youssef L Bennani, Arthur A Hancock

文献索引：Bioorg. Med. Chem. Lett. 13(13) , 2131-5, (2003)

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摘要

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.

相关化合物

  • 对甲苯磺酸3-丁炔酯

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