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Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist |
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| Authors: | Hong Qingmei Bakshi Raman K Palucki Brenda L Park Min K Ye Zhixiong He Shuwen Pollard Patrick G Sebhat Iyassu K Liu Jian Guo Liangqin Cashen Doreen E Martin William J Weinberg David H MacNeil Tanya Tang Rui Tamvakopoulos Constantin Peng Qianping Miller Randy R Stearns Ralph A Chen Howard Y Chen Airu S Strack Alison M Fong Tung M MacIntyre D Euan Wyvratt Matthew J Nargund Ravi P |
| Institution: | a Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA b Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 07065-0900, USA c Department of Obesity Research, Merck Research Laboratories, Rahway, NJ 07065-0900, USA d Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ 07065-0900, USA |
| Abstract: | We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models. |
| Keywords: | Melanocortin subtype-4 receptor MC4R Partial agonist Urea piperazine Erectile dysfunction Obesity |
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