2. Academic Validation
  3. Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2

  • Bioorg Med Chem Lett. 2004 Oct 4;14(19):4879-82. doi: 10.1016/j.bmcl.2004.07.034.
Anil Vasudevan 1,  Dariusz Wodka,  Mary K Verzal,  Andrew J Souers,  Ju Gao,  Sevan Brodjian,  Dennis Fry,  Brian Dayton,  Kennan C Marsh,  Lisa E Hernandez,  Christopher A Ogiela,  Christine A Collins,  Philip R Kym
Affiliations

Affiliation

  • 1 Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. anil.vasudevan@abbott.com
PMID: 15341943 DOI: 10.1016/j.bmcl.2004.07.034
Abstract

The continued SAR investigation of 2-amino-8-alkoxy quinolines as melanin concentrating hormone receptor-1 (MCHr1) antagonists is reported. Prior hit-to-lead efforts resulted in the identification of 1 as a robust MCHr1 antagonist. Further delineation of the structural parameters essential for MCHr1-binding affinity of this class of nontraditional GPCR ligands resulted in the identification of compounds such as 33, 34 and 37, which demonstrate single digit nanomolar antagonism of MCHr1-mediated CA(2+) release. The synthesis and biological evaluation of these compounds are reported.

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