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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2004.03.014
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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez... doi:10.1016/j.bmcl.2004.03.014
Date Deposited:	14 Dec 2009 13:54
Last Modified:	31 Jan 2013 01:07
URI:	https://oak.novartis.com/id/eprint/762