том 44 издание 26 страницы 4641-4649

Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues

Тип публикацииJournal Article
Дата публикации2001-11-16
scimago Q1
wos Q1
БС1
SJR1.801
CiteScore11.5
Impact factor6.8
ISSN00222623, 15204804
Drug Discovery
Molecular Medicine
Краткое описание
A series of substituted oxindole derivatives was synthesized and evaluated for growth hormone (GH) releasing activity using cultured rat pituitary cells. (+)-6-Carbamoyl-3-(2-chlorophenyl)-(2-diethylaminoethyl)-4-trifluoromethyloxindole (SM-130686, 37S) was found to have potent activity (EC(50) = 3.0 nM), while the other enantiomer 37R had reduced activity. The absolute configuration of 37S was confirmed by X-ray crystallographic analysis. Compound 37S showed a good pharmacokinetic profile in rats with 28% oral bioavailability at 10 mg/kg and excellent in vivo activity as evidenced by a significant weight gain after 4 days of oral administration at 10 mg/kg twice a day. Compound 37S displaced the binding of (35)S-MK-677 to human GHS-R with an IC(50) value of 1.2 +/- 0.2 nM.
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ГОСТ |
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Tokunaga T. et al. Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues // Journal of Medicinal Chemistry. 2001. Vol. 44. No. 26. pp. 4641-4649.
ГОСТ со всеми авторами (до 50) Скопировать
Tokunaga T., Hume W. E., UMEZOME T., OKAZAKI K., Ueki Y., KUMAGAI K., Hourai S., Nagamine J., Seki H., Taiji M., Noguchi H., Nagata R. Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues // Journal of Medicinal Chemistry. 2001. Vol. 44. No. 26. pp. 4641-4649.
RIS |
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TY - JOUR
DO - 10.1021/jm0103763
UR - https://doi.org/10.1021/jm0103763
TI - Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues
T2 - Journal of Medicinal Chemistry
AU - Tokunaga, Teruhisa
AU - Hume, W. Ewan
AU - UMEZOME, Takashi
AU - OKAZAKI, Kazuhiko
AU - Ueki, Yasuyuki
AU - KUMAGAI, Kazuo
AU - Hourai, Shinji
AU - Nagamine, Jun
AU - Seki, Hitoshi
AU - Taiji, Mutsuo
AU - Noguchi, Hiroshi
AU - Nagata, Ryu
PY - 2001
DA - 2001/11/16
PB - American Chemical Society (ACS)
SP - 4641-4649
IS - 26
VL - 44
PMID - 11741481
SN - 0022-2623
SN - 1520-4804
ER -
BibTex |
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BibTex (до 50 авторов) Скопировать
@article{2001_Tokunaga,
author = {Teruhisa Tokunaga and W. Ewan Hume and Takashi UMEZOME and Kazuhiko OKAZAKI and Yasuyuki Ueki and Kazuo KUMAGAI and Shinji Hourai and Jun Nagamine and Hitoshi Seki and Mutsuo Taiji and Hiroshi Noguchi and Ryu Nagata},
title = {Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues},
journal = {Journal of Medicinal Chemistry},
year = {2001},
volume = {44},
publisher = {American Chemical Society (ACS)},
month = {nov},
url = {https://doi.org/10.1021/jm0103763},
number = {26},
pages = {4641--4649},
doi = {10.1021/jm0103763}
}
MLA
Цитировать
Tokunaga, Teruhisa, et al. “Oxindole Derivatives as Orally Active Potent Growth Hormone Secretagogues.” Journal of Medicinal Chemistry, vol. 44, no. 26, Nov. 2001, pp. 4641-4649. https://doi.org/10.1021/jm0103763.