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Discovery of a spiroindane based compound as a potent,selective, orally bioavailable melanocortin subtype-4 receptor agonist |
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| Authors: | Shuwen He Zhixiong Ye Peter H. Dobbelaar Iyassu K. Sebhat Liangqin Guo Jian Liu Tianying Jian Yingjie Lai Christopher L. Franklin Raman K. Bakshi James P. Dellureficio Qingmei Hong Nancy N. Tsou Richard G. Ball Doreen E. Cashen William J. Martin David H. Weinberg Tanya MacNeil Rui Tang Constantin Tamvakopoulos Ravi P. Nargund |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA;2. Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 07065-0900, USA;3. Department of Obesity Research, Merck Research Laboratories, Rahway, NJ 07065-0900, USA;4. Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ 07065-0900, USA |
| Abstract: | We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models. |
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