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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: foster ac. J Med Chem. 2007 Nov 1;50(22):5249-52. doi: 10.1021/jm070806a. Epub 2007 Oct 5. J Med Chem. 2007. PMID: 17918824
Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines.
Tucci FC, White NS, Markison S, Joppa M, Tran JA, Fleck BA, Madan A, Dyck BP, Parker J, Pontillo J, Arellano LM, Marinkovic D, Jiang W, Chen CW, Gogas KR, Goodfellow VS, Saunders J, Foster AC, Chen C. Tucci FC, et al. Among authors: foster ac. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4389-95. doi: 10.1016/j.bmcl.2005.06.071. Bioorg Med Chem Lett. 2005. PMID: 16098742
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: foster ac. 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
Propionylpiperazines as human melanocortin-4 receptor ligands.
Chen CW, Tran JA, Jiang W, Tucci FC, Arellano M, Wen J, Fleck BA, Marinkovic D, White NS, Pontillo J, Saunders J, Madan A, Foster AC, Chen C. Chen CW, et al. Among authors: foster ac. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4800-3. doi: 10.1016/j.bmcl.2006.06.075. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824757
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Tran JA, Tucci FC, Jiang W, Marinkovic D, Chen CW, Arellano M, Markison S, Fleck BA, Wen J, White NS, Pontillo J, Saunders J, Marks D, Hoare SR, Madan A, Foster AC, Chen C. Tran JA, et al. Among authors: foster ac. Bioorg Med Chem. 2007 Aug 1;15(15):5166-76. doi: 10.1016/j.bmc.2007.05.026. Epub 2007 May 17. Bioorg Med Chem. 2007. PMID: 17544282
184 results