Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis

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Abstract

-4-Amino-2-arylbutylbenzamides such as 1 were identified as micromolar MCH 1 receptor (MCH1R) antagonists via screening using a scintillation proximity assay based on [125I]-MCH binding to recombinant, human MCH1R. Subsequent lead optimization efforts using solid-phase parallel synthesis resulted in the defined structure-activity relationships and the identification of 4-amino-2-biarylbutylureas, such as 11g, as potent single digit nanomolar MCH1R antagonists. © 2005 Elsevier Ltd. All rights reserved.

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Guo, T., Hunter, R. C., Gu, H., Rokosz, L. L., Stauffer, T. M., & Hobbs, D. W. (2005). Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis. Bioorganic and Medicinal Chemistry Letters, 15(16), 3691–3695. https://doi.org/10.1016/j.bmcl.2005.05.039

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