2. Academic Validation
  3. Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2

Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2

  • J Med Chem. 2011 Apr 14;54(7):2351-8. doi: 10.1021/jm101501b.
Scott E Wolkenberg 1,  Zhijian Zhao,  Catherine Thut,  Jill W Maxwell,  Terrence P McDonald,  Fumi Kinose,  Michael Reilly,  Craig W Lindsley,  George D Hartman
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486, United States. scott_wolkenberg@merck.com
PMID: 21395312 DOI: 10.1021/jm101501b
Abstract

Agonists of Somatostatin Receptor subtype 2 (sst(2)) have been proposed as therapeutics for the treatment of proliferative diabetic retinopathy and exudative age-related macular degeneration. An HTS screen identified 2-quinolones as weak agonists of sst(2), and these were optimized to provide small molecules with sst(2) binding and functional potency comparable to peptide agonists. Agonist 21 was shown to inhibit rat growth hormone secretion following systemic administration and to inhibit ocular neovascular lesion formation after local administration.

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