Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives

Bioorganic & Medicinal Chemistry Letters
Yoshio OginoTakehiro Fukami

Abstract

Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists (2 and 3). By optimizing substituents on the benzimidazole core part of the lead compound 5a, we were able to develop a potent, orally available, and brain-penetrable Y5 selective antagonist (5k).

Citations

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Jan 19, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Emre MenteşeBahittin Kahveci
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Feb 27, 2009·Bioorganic & Medicinal Chemistry Letters·Toshihiro SakamotoLihu Yang

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