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Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands |
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| Authors: | Qingmei Hong Raman K Bakshi James Dellureficio Shuwen He Zhixiong Ye Peter H Dobbelaar Iyassu K Sebhat Liangqin Guo Jian Liu Tianying Jian Rui Tang Rubana N Kalyani Tanya MacNeil Aurawan Vongs Charles I Rosenblum David H Weinberg Qingping Peng Constantin Tamvakopoulos Randy R Miller Ralph A Stearns Ravi P Nargund |
| Institution: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA;2. Department of Obesity Research Pharmacology, Merck Research Laboratories, Rahway, NJ 07065-0900, USA;3. Department of Drug Metabolism, Merck Research Laboratories, Rahway, NJ 07065-0900, USA;4. Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 07065-0900, USA |
| Abstract: | Design, syntheses and structure–activity relationships of N-acetylated piperazine privileged structures containing MC4R agonist compounds were described. The most potent derivatives were low nM MC4R selective full agonists. Several compounds from the series had modest pharmacokinetic properties. |
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