Synthesis and SAR of highly potent dual 5-HT 1A and 5-HT 1B antagonists as potential antidepressant drugs

…, W Hornberger, CW Hutchins, A Möller, R Müller…

文献索引：Kling, Andreas; Lange, Udo E. W.; Mack, Helmut; Bakker, Margot H. M.; Drescher, Karla U.; Hornberger, Wilfried; Hutchins, Charles W.; Moeller, Achim; Mueller, Reinhold; Schmidt, Martin; Unger, Liliane; Wicke, Karsten; Schellhaas, Kurt; Steiner, Gerd Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 24 p. 5567 - 5573

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被引用次数: 22

摘要

Novel 5-HT1 autoreceptor ligands based on the N-4-aryl-piperazinyl-N′-ethyl-5, 6, 7, 8- tetrahydropyrido [4′, 3′: 4, 5] thieno [2, 3-d] pyrimidin-4 (3H)-one core are described. Aiming at antidepressants with a novel mode of action our objective was to identify potent antagonists showing balanced affinities and high selectivity for the 5-HT1A and 5-HT1B receptors. Strategies for the development of dual 5-HT1A and 5-HT1B antagonists based ...