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Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives
Matthew J Fisher1, Ryan T Backer, Iván Collado
1Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46258, USA. fisher_matthew_j@lilly.com
Abstract:
Replacement of the aryl piperazine moiety in compound 1 with a variety of substituted benzylic piperazines (6) yields compounds that afford melanocortin receptor 4 (MCR4) activity. Analogs with ortho substitution on the aromatic ring afforded the highest affinity. Resolution of the stereocenter of the benzylic piperazine based privileged structure revealed that the R-enantiomer was more active.
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