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

Yoshio Ogino; Norikazu Ohtake; Yoshikazu Nagae; Kenji Matsuda; Makoto Ishikawa; Minoru Moriya; Maki Kanesaka; Yuko Mitobe; Junko Ito; Tetsuya Kanno; Akane Ishihara; Hisashi Iwaasa; Tomoyuki Ohe; Akio Kanatani; Takehiro Fukami

doi:10.1016/j.bmcl.2008.08.021

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

Yoshio Ogino, Norikazu Ohtake, Yoshikazu Nagae, Kenji Matsuda, Makoto Ishikawa, Minoru Moriya, Maki Kanesaka, Yuko Mitobe, Junko Ito, Tetsuya Kanno, Akane Ishihara, Hisashi Iwaasa, Tomoyuki Ohe, Akio Kanatani, Takehiro Fukami

研究成果: Article › 査読

15 被引用数 (Scopus)

抄録

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

本文言語	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
号	18
DOI	https://doi.org/10.1016/j.bmcl.2008.08.021
出版ステータス	Published - 2008 9 15
外部発表	はい

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

文献へのアクセス

10.1016/j.bmcl.2008.08.021

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。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル

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

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. / Ogino, Yoshio; Ohtake, Norikazu; Nagae, Yoshikazu; Matsuda, Kenji; Ishikawa, Makoto; Moriya, Minoru; Kanesaka, Maki; Mitobe, Yuko; Ito, Junko; Kanno, Tetsuya; Ishihara, Akane; Iwaasa, Hisashi; Ohe, Tomoyuki; Kanatani, Akio; Fukami, Takehiro.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 18, 15.09.2008, p. 4997-5001.

研究成果: Article › 査読

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, vol. 18, no. 18, pp. 4997-5001. https://doi.org/10.1016/j.bmcl.2008.08.021

Ogino, Yoshio ; Ohtake, Norikazu ; Nagae, Yoshikazu ; Matsuda, Kenji ; Ishikawa, Makoto ; Moriya, Minoru ; Kanesaka, Maki ; Mitobe, Yuko ; Ito, Junko ; Kanno, Tetsuya ; Ishihara, Akane ; Iwaasa, Hisashi ; Ohe, Tomoyuki ; Kanatani, Akio ; Fukami, Takehiro. / 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. In: Bioorganic and Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 18. pp. 4997-5001.

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AU - Kanno, Tetsuya

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