Design, Synthesis, and Evaluation of Novel 3,6-Diaryl-4-aminoalkoxyquinolines as Selective Agonists of Somatostatin Receptor Subtype 2

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• 作者：Scott E. Wolkenberg ; Zhijian Zhao ; Catherine Thut ; Jill W. Maxwell ; Terrence P. McDonald ; Fumi Kinose ; Michael Reilly ; Craig W. Lindsley ; George D. Hartman
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：April 14, 2011
• 年：2011
• 卷：54
• 期：7
• 页码：2351-2358
• 全文大小：915K
• 年卷期：v.54,no.7(April 14, 2011)
• ISSN：1520-4804

文摘

Agonists of somatostatin receptor subtype 2 (sst₂) 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 sst₂, and these were optimized to provide small molecules with sst₂ 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.