Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

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• 作者：Palucki ; Brenda L. ; Park ; Min K. ; Nargund ; Ravi P. ; Ye ; Zhixiong ; Sebhat ; Iyassu K. ; Pollard ; Patrick G. ; et. al.
• 关键词：Melanocortin ; Obesity ; Sexual dysfunction
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：January 3, 2005
• 年：2005
• 卷：15
• 期：1
• 页码：171-175
• 全文大小：291 K

文摘

We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.