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). Crown
| Original language | English |
|---|---|
| Pages (from-to) | 5010-5014 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 18 |
| Issue number | 18 |
| DOIs | |
| Publication status | Published - 2008 Sep 15 |
| Externally published | Yes |
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Keywords
- Antagonist
- Anti-obesity
- Benzimidazole
- Neuropeptide Y
- Y5 receptor
ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science
Cite this
Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists : 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives. / Ogino, Yoshio; Ohtake, Norikazu; Nagae, Yoshikazu; Matsuda, Kenji; Moriya, Minoru; Suga, Takuya; Ishikawa, Makoto; 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. 5010-5014.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists
T2 - 2-{3-Oxospiro[isobenzofuran-1(3H),4′-piperidin]-1′-yl}benzimidazole derivatives
AU - Ogino, Yoshio
AU - Ohtake, Norikazu
AU - Nagae, Yoshikazu
AU - Matsuda, Kenji
AU - Moriya, Minoru
AU - Suga, Takuya
AU - Ishikawa, Makoto
AU - Kanesaka, Maki
AU - Mitobe, Yuko
AU - Ito, Junko
AU - Kanno, Tetsuya
AU - Ishihara, Akane
AU - Iwaasa, Hisashi
AU - Ohe, Tomoyuki
AU - Kanatani, Akio
AU - Fukami, Takehiro
PY - 2008/9/15
Y1 - 2008/9/15
N2 - 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). Crown
AB - 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). Crown
KW - Antagonist
KW - Anti-obesity
KW - Benzimidazole
KW - Neuropeptide Y
KW - Y5 receptor
UR - http://www.scopus.com/inward/record.url?scp=51349162920&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=51349162920&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2008.08.018
DO - 10.1016/j.bmcl.2008.08.018
M3 - Article
C2 - 18723347
AN - SCOPUS:51349162920
VL - 18
SP - 5010
EP - 5014
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 18
ER -