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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 |
| Institution: | 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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