2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.
作者信息
Bergauer Markus, Hübner Harald, Gmeiner Peter
机构信息
Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052 Erlangen, Germany.
出版信息
Bioorg Med Chem Lett. 2002 Aug 5;12(15):1937-40. doi: 10.1016/s0960-894x(02)00316-5.
Abstract
Solution-phase synthesis and a solid-phase supported approach to piperazinylmethyl substituted pyrroles are described. Receptor binding studies and the measurement of D4 ligand efficacy led to the ethynylpyrrole 1d (FAUC 356) exerting selective D4 binding and substantial ligand efficacy (66%, EC(50)=1.9nM). This activity profile might be of interest for the treatment of ADHD.
摘要
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