Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists
Tetsuji Saito
1
,
Tetsuo Obitsu
1
,
Hiroshi KOHNO
1
,
I. Sugimoto
1
,
Takeshi Matsushita
1
,
Taihei Nishiyama
1
,
Tomoko Hirota
1
,
Hiroyuki Takeda
1
,
Naoya Matsumura
1
,
Sonoko Ueno
1
,
Akihiro Kishi
1
,
Yoshifumi Kagamiishi
1
,
Hisao Nakai
1
,
Yoshikazu Takaoka
1
1
Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan.
|
Publication type: Journal Article
Publication date: 2012-01-01
scimago Q2
wos Q1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3.0
ISSN: 09680896, 14643391
PubMed ID:
22196514
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
To identify structurally novel corticotropin-releasing factor 1 (CRF(1)) receptor antagonists, a series of bicyclic core analogs pyrrolo[1,2-b]pyridazines and pyrrolo[2,1-f]triazin-4(3H)-ones, which were designed based on a monocyclic core antagonist, was synthesized and evaluated. Among the compounds tested, 2-difluoromethoxy-4-methylpyridin-5-yl analog 27 was found to show efficacy in a dose-dependent manner in an elevated plus maze test in rats. The discovery process and structure-activity relationship is presented.
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17
Total citations:
17
Citations from 2025:
2
(11.76%)
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GOST
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Saito T. et al. Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists // Bioorganic and Medicinal Chemistry. 2012. Vol. 20. No. 2. pp. 1122-1138.
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Saito T., Obitsu T., KOHNO H., Sugimoto I., Matsushita T., Nishiyama T., Hirota T., Takeda H., Matsumura N., Ueno S., Kishi A., Kagamiishi Y., Nakai H., Takaoka Y. Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists // Bioorganic and Medicinal Chemistry. 2012. Vol. 20. No. 2. pp. 1122-1138.
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TY - JOUR
DO - 10.1016/j.bmc.2011.11.015
UR - https://doi.org/10.1016/j.bmc.2011.11.015
TI - Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists
T2 - Bioorganic and Medicinal Chemistry
AU - Saito, Tetsuji
AU - Obitsu, Tetsuo
AU - KOHNO, Hiroshi
AU - Sugimoto, I.
AU - Matsushita, Takeshi
AU - Nishiyama, Taihei
AU - Hirota, Tomoko
AU - Takeda, Hiroyuki
AU - Matsumura, Naoya
AU - Ueno, Sonoko
AU - Kishi, Akihiro
AU - Kagamiishi, Yoshifumi
AU - Nakai, Hisao
AU - Takaoka, Yoshikazu
PY - 2012
DA - 2012/01/01
PB - Elsevier
SP - 1122-1138
IS - 2
VL - 20
PMID - 22196514
SN - 0968-0896
SN - 1464-3391
ER -
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BibTex (up to 50 authors)
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@article{2012_Saito,
author = {Tetsuji Saito and Tetsuo Obitsu and Hiroshi KOHNO and I. Sugimoto and Takeshi Matsushita and Taihei Nishiyama and Tomoko Hirota and Hiroyuki Takeda and Naoya Matsumura and Sonoko Ueno and Akihiro Kishi and Yoshifumi Kagamiishi and Hisao Nakai and Yoshikazu Takaoka},
title = {Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists},
journal = {Bioorganic and Medicinal Chemistry},
year = {2012},
volume = {20},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/j.bmc.2011.11.015},
number = {2},
pages = {1122--1138},
doi = {10.1016/j.bmc.2011.11.015}
}
Cite this
MLA
Copy
Saito, Tetsuji, et al. “Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists.” Bioorganic and Medicinal Chemistry, vol. 20, no. 2, Jan. 2012, pp. 1122-1138. https://doi.org/10.1016/j.bmc.2011.11.015.