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

  • Guo T
  • Hunter R
  • Gu H
 et al. 
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-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.

Author-supplied keywords

  • MCH
  • MCH1R antagonists
  • Obesity
  • Solid-phase parallel synthesis

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  • Tao Guo

  • Rachael C. Hunter

  • Huizhong Gu

  • Laura L. Rokosz

  • Tara M. Stauffer

  • Doug W. Hobbs

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