Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists
Тип публикации: Journal Article
Дата публикации: 2018-05-01
SCImago Q2
WOS Q1
БС1
SJR: 0.582
CiteScore: 6.7
Impact factor: 3
ISSN: 09680896, 14643391
PubMed ID:
29486951
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
The design and synthesis of a novel class of 7-azaspiro[3.5]nonane GPR119 agonists are described. In this series, optimization of the right piperidine N-capping group (R2) and the left aryl group (R3) led to the identification of compound 54g as a potent GPR119 agonist. Compound 54g showed a desirable PK profile in Sprague-Dawley (SD) rats and a favorable glucose lowering effect in diabetic rats.
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ГОСТ
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Matsuda D. et al. Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists // Bioorganic and Medicinal Chemistry. 2018. Vol. 26. No. 8. pp. 1832-1847.
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Matsuda D., Kawamura M., Kobashi Y., Shiozawa F., Suga Y., Fusegi K., Nishimoto S., Kimura K., Miyoshi M., Takayama N., Kakinuma H., Ohtake N. Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists // Bioorganic and Medicinal Chemistry. 2018. Vol. 26. No. 8. pp. 1832-1847.
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TY - JOUR
DO - 10.1016/j.bmc.2018.02.032
UR - https://doi.org/10.1016/j.bmc.2018.02.032
TI - Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists
T2 - Bioorganic and Medicinal Chemistry
AU - Matsuda, Daisuke
AU - Kawamura, Madoka
AU - Kobashi, Yohei
AU - Shiozawa, Fumiyasu
AU - Suga, Youichirou
AU - Fusegi, Keiko
AU - Nishimoto, Shinichi
AU - Kimura, Kayo
AU - Miyoshi, Masako
AU - Takayama, Noriko
AU - Kakinuma, Hiroyuki
AU - Ohtake, Norikazu
PY - 2018
DA - 2018/05/01
PB - Elsevier
SP - 1832-1847
IS - 8
VL - 26
PMID - 29486951
SN - 0968-0896
SN - 1464-3391
ER -
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@article{2018_Matsuda,
author = {Daisuke Matsuda and Madoka Kawamura and Yohei Kobashi and Fumiyasu Shiozawa and Youichirou Suga and Keiko Fusegi and Shinichi Nishimoto and Kayo Kimura and Masako Miyoshi and Noriko Takayama and Hiroyuki Kakinuma and Norikazu Ohtake},
title = {Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists},
journal = {Bioorganic and Medicinal Chemistry},
year = {2018},
volume = {26},
publisher = {Elsevier},
month = {may},
url = {https://doi.org/10.1016/j.bmc.2018.02.032},
number = {8},
pages = {1832--1847},
doi = {10.1016/j.bmc.2018.02.032}
}
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MLA
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Matsuda, Daisuke, et al. “Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists.” Bioorganic and Medicinal Chemistry, vol. 26, no. 8, May. 2018, pp. 1832-1847. https://doi.org/10.1016/j.bmc.2018.02.032.
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