Turner Sean C, Esbenshade Timothy A, Bennani Youssef L, Hancock Arthur A
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, 60064, Abbott Park, IL, USA.
Bioorg Med Chem Lett. 2003 Jul 7;13(13):2131-5. doi: 10.1016/s0960-894x(03)00356-1.
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.
本文描述了新型人H(3)受体环庚喹啉拮抗剂的合成及生物学评价。研究了在11位带有氨基取代基或炔烃连接基的两个系列化合物。描述了氨基取代基的修饰、链长的优化以及构象限制的影响。发现了几种对H(3)受体具有高亲和力和选择性的化合物。
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