4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

Jinlong Jiang, Peter Lin, Myle Hoang, Lehua Chang, Carina Tan, Scott Feighner, Oksana C. Palyha, Donna L. Hreniuk, Jie Pan, Andreas W. Sailer, Nancy R. Morin, Douglas J. MacNeil, Andrew D. Howard, Lex H.T. Van der Ploeg, Mark T. Goulet, Robert J. DeVita

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Structure-activity relationships of a 4-aminoquinoline MCH1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated.

Original languageEnglish
Pages (from-to)5275-5279
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number20
DOIs
StatePublished - 15 Oct 2006
Externally publishedYes

Keywords

  • Antagonist
  • Anxiety
  • Depression
  • MCH
  • Melanin-concentrating hormone
  • Obesity
  • Quinoline

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