Aryl piperazine melanocortin MC4 receptor agonists

…, R Summers, J Hermann, T Baker, M Cismowski…

文献索引：Dyck, Brian; Parker, Jessica; Phillips, Teresa; Carter, Lee; Murphy, Brian; Summers, Robin; Hermann, Julia; Baker, Tracy; Cismowski, Mary; Saunders, John; Goodfellow, Val Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 21 p. 3793 - 3796

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被引用次数: 55

摘要

Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC50= 24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or other melancortin receptors.