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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: marinkovic d. 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: marinkovic d. 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
4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.
Chen C, Pontillo J, Fleck BA, Gao Y, Wen J, Tran JA, Tucci FC, Marinkovic D, Foster AC, Saunders J. Chen C, et al. Among authors: marinkovic d. J Med Chem. 2004 Dec 30;47(27):6821-30. doi: 10.1021/jm049278i. J Med Chem. 2004. PMID: 15615531
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: marinkovic d. 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
200 results