Discovery and optimization of a series of carbazole ureas as NPY5 antagonists for the treatment of obesity

…, DR Brittain, D Carroll, S Chapman…

Index: Block, Michael H.; Boyer, Scott; Brailsford, Wayne; Brittain, David R.; Carroll, Debra; Chapman, Steve; Clarke, David S.; Donald, Craig S.; Foote, Kevin M.; Godfrey, Linda; Ladner, Anthony; Marsham, Peter R.; Masters, David J.; Mee, Christine D.; O'Donovan, Michael R.; Pease, J. Elizabeth; Pickup, Adrian G.; Rayner, John W.; Roberts, Andrew; Schofield, Paul; Suleman, Abid; Turnbull, Andrew V. Journal of Medicinal Chemistry, 2002 , vol. 45, # 16 p. 3509 - 3523

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Citation Number: 61

Abstract

The hypothesis that antagonists of the neuropeptide Y5 receptor would provide safe and effective appetite suppressants for the treatment of obesity has prompted vigorous research to identify suitable compounds. We discovered a series of acylated aminocarbazole derivatives (eg, 3a) that are potent and selective Y5 antagonists, representing interesting starting points but suffering from poor bioavailability and concerns about potential toxicity ...