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Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.

Authors
  • Souers, Andrew J
  • Wodka, Dariusz
  • Gao, Ju
  • Lewis, Jared C
  • Vasudevan, Anil
  • Gentles, Robert
  • Brodjian, Sevan
  • Dayton, Brian
  • Ogiela, Christopher A
  • Fry, Dennis
  • Hernandez, Lisa E
  • Marsh, Kennan C
  • Collins, Christine A
  • Kym, Philip R
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Oct 04, 2004
Volume
14
Issue
19
Pages
4873–4877
Identifiers
PMID: 15341942
Source
Medline
License
Unknown

Abstract

A high-throughput screen was performed in order to identify chemotypes that are bound by the melanin concentrating hormone receptor-1 (MCHr1). A novel 2-amino-8-alkoxyquinoline compound (1) was identified and subsequently optimized using a parallel and automated procedure for the rapid production of multiple analogs. The structure-activity relationships that emerged from this effort are described, along with selected pharmacokinetic parameters of compound (d)-61 when dosed orally in diet-induced obese mice.

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