| 16777413 |
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: Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4674-8. Epub 2006 Jun 13.
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or beta-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability. |
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