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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]azulen derivatives as neuropeptide Y Y5 receptor antagonists.

Rueeger, Heinrich and Gerspacher, Marc and Buehlmayer, Peter and Rigollier, Pascal and Yamaguchi, Yasuchika and Schmidlin, Tibur and Whitebread, Steven and Nuesslein-Hildesheim, Barbara and Nick, Hanspeter and Cricione, Leoluca (2004) 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]azulen derivatives as neuropeptide Y Y5 receptor antagonists. Bioorganic & Medicinal Chemistry Letters, 14 (10). pp. 2451-2457. ISSN 0960-894X

Abstract

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 bioavailable NPY Y5 receptor antagonists.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: NPY Y5 antagonists; Neuropetide Y receptors
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Date Deposited: 14 Dec 2009 13:54
Last Modified: 31 Jan 2013 01:07
URI: https://oak.novartis.com/id/eprint/762

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