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Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Chen C, Jiang W, Tucci F, Tran JA, Fleck BA, Hoare SR, Joppa M, Markison S, Wen J, Sai Y, Johns M, Madan A, Chen T, Chen CW, Marinkovic D, Arellano M, Saunders J, Foster AC. Chen C, et al. Among authors: arellano m. J Med Chem. 2007 Nov 1;50(22):5249-52. doi: 10.1021/jm070806a. Epub 2007 Oct 5. J Med Chem. 2007. PMID: 17918824
Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Pontillo J, Tran JA, Arellano M, Fleck BA, Huntley R, Marinkovic D, Lanier M, Nelson J, Parker J, Saunders J, Tucci FC, Jiang W, Chen CW, White NS, Foster AC, Chen C. Pontillo J, et al. Among authors: arellano m. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4417-23. doi: 10.1016/j.bmcl.2004.06.059. Bioorg Med Chem Lett. 2004. PMID: 15357964
Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Jiang W, Tucci FC, Chen CW, Arellano M, Tran JA, White NS, Marinkovic D, Pontillo J, Fleck BA, Wen J, Saunders J, Madan A, Foster AC, Chen C. Jiang W, et al. Among authors: arellano m. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4674-8. doi: 10.1016/j.bmcl.2006.05.088. Epub 2006 Jun 13. Bioorg Med Chem Lett. 2006. PMID: 16777413
296 results