Discovery and SAR of potent, orally available and brain-penetrable 5, 6-dihydro-4H-3-thia-1-aza-benzo [e] azulen-and 4, 5-dihydro-6-oxa-3-thia-1-aza-benzo [e] …

…, S Whitebread, B Nuesslein-Hildesheim, H Nick…

文献索引：Rueeger, Heinrich; Gerspacher, Marc; Buehlmayer, Peter; Rigollier, Pascal; Yamaguchi, Yasuchika; Schmidlin, Tibur; Whitebread, Steven; Nuesslein-Hildesheim, Barbara; Nick, Hanspeter; Cricione, Leoluca Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2451 - 2457

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被引用次数: 19

摘要

Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5, 6- dihydro-4H-3-thia-1-aza-benzo [e] azulen-2-yl)-piperidin-4-ylmethyl-amino and (4, 5-dihydro- 6-oxa-3-thia-1-aza-benzo [e] azulen-2-yl)-piperidin-4-ylmethyl-amino derivatives. Both classes of compounds are capable of delivering potent and selective orally and centrally ...