Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594589 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
Optimization of our HTS hit 1, mainly focused on modification at the C-2 position of the benzimidazole core, is described. Elimination of the flexible and metabolically labile -S-CH2- part and utilization of less lipophilic pyridone substructure led to identification of novel NPY Y5 receptor antagonists 6, which have low to sub-nanomolar Y5 receptor binding affinity with improved CYP450 inhibition profiles, good solubilities and high metabolic stabilities.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yuusuke Tamura, Naoki Omori, Naoki Kouyama, Yuji Nishiura, Kyouhei Hayashi, Kana Watanabe, Yukari Tanaka, Takeshi Chiba, Hideo Yukioka, Hiroki Sato, Takayuki Okuno,