Adamantyl thioureas as soluble epoxide hydrolase inhibitors
Тип публикации: Journal Article
Дата публикации: 2018-07-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
29803731
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
A series of inhibitors of the soluble epoxide hydrolase (sEH) containing one or two thiourea groups has been developed. Inhibition potency of the described compounds ranges from 50 μM to 7.2 nM. 1,7-(Heptamethylene)bis[(adamant-1-yl)thiourea] (6f) was found to be the most potent sEH inhibitor, among the thioureas tested. The inhibitory activity of the thioureas against the human sEH is closer to the value of activity against rat sEH rather than murine sEH. While being less active, thioureas are up to 7-fold more soluble than ureas, which makes them more bioavailable and thus promising as sEH inhibitors.
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ГОСТ
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Morisseau C. et al. Adamantyl thioureas as soluble epoxide hydrolase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2018. Vol. 28. No. 13. pp. 2302-2313.
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Morisseau C., Pitushkin D., Karlov D., Fayzullin R. R., Butov G. M., Hammock B. D. Adamantyl thioureas as soluble epoxide hydrolase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2018. Vol. 28. No. 13. pp. 2302-2313.
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TY - JOUR
DO - 10.1016/j.bmcl.2018.05.024
UR - https://doi.org/10.1016/j.bmcl.2018.05.024
TI - Adamantyl thioureas as soluble epoxide hydrolase inhibitors
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Morisseau, Christophe
AU - Pitushkin, Dmitry
AU - Karlov, Dmitry
AU - Fayzullin, Robert R
AU - Butov, Gennady M
AU - Hammock, Bruce D.
PY - 2018
DA - 2018/07/01
PB - Elsevier
SP - 2302-2313
IS - 13
VL - 28
PMID - 29803731
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2018_Morisseau,
author = {Christophe Morisseau and Dmitry Pitushkin and Dmitry Karlov and Robert R Fayzullin and Gennady M Butov and Bruce D. Hammock},
title = {Adamantyl thioureas as soluble epoxide hydrolase inhibitors},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2018},
volume = {28},
publisher = {Elsevier},
month = {jul},
url = {https://doi.org/10.1016/j.bmcl.2018.05.024},
number = {13},
pages = {2302--2313},
doi = {10.1016/j.bmcl.2018.05.024}
}
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MLA
Скопировать
Morisseau, Christophe, et al. “Adamantyl thioureas as soluble epoxide hydrolase inhibitors.” Bioorganic and Medicinal Chemistry Letters, vol. 28, no. 13, Jul. 2018, pp. 2302-2313. https://doi.org/10.1016/j.bmcl.2018.05.024.
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