抜粋
Syntheses and structure-activity relationships of a novel class of 2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists are described. Optimization of the lead compound 2a by incorporating substituents into the 5-position or into both the 5- and 6-positions of the benzimidazole core part led to the identification of 5-(5-methyl-1,2,4-oxadiazol-2-yl)benzimidazole (2r: IC50 = 3.3 nM) and 5-(2-methyltetrazol-5-yl)benzimidazole (2u: IC50 = 5.9 nM), both of which are potent, selective, and orally bioavailable Y5 receptor antagonists. Crown
| 元の言語 | English |
|---|---|
| ページ（範囲） | 4997-5001 |
| ページ数 | 5 |
| ジャーナル | Bioorganic and Medicinal Chemistry Letters |
| 巻 | 18 |
| 発行部数 | 18 |
| DOI | |
| 出版物ステータス | Published - 2008 9 15 |
| 外部発表 | Yes |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
フィンガープリント Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists' の研究トピックを掘り下げます。これらはともに一意のフィンガープリントを構成します。
これを引用
Ogino, Y., Ohtake, N., Nagae, Y., Matsuda, K., Ishikawa, M., Moriya, M., Kanesaka, M., Mitobe, Y., Ito, J., Kanno, T., Ishihara, A., Iwaasa, H., Ohe, T., Kanatani, A., & Fukami, T. (2008). Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1′-cyclohexan]-4′-yl]benzimidazole NPY Y5 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 18(18), 4997-5001. https://doi.org/10.1016/j.bmcl.2008.08.021