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2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists |
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| Authors: | Palucki Brenda L Park Min K Nargund Ravi P Tang Rui MacNeil Tanya Weinberg David H Vongs Aurawan Rosenblum Charles I Doss George A Miller Randall R Stearns Ralph A Peng Qianping Tamvakopoulos Constantin Van der Ploeg Lex H T Patchett Arthur A |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. brenda_palucki@merck.com |
| Abstract: | We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. The 5- and 6-alkylated piperazine compounds exhibit low bioactivation potential as measured by covalent binding in microsome preparations. |
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