Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors
1
Institute of Microbial Chemistry, Tokyo, 3-14-23 Kamiosaki, Shinagawa-ku, Tokyo 141-0021, Japan
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Тип публикации: Journal Article
Дата публикации: 2010-10-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
20728352
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
Pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase (OSC) inhibitors 3 and 4 were discovered by conducting a virtual screening, a docking study based on the crystallographic structure of OSC, and biological assays. The hit rate of the assays was increased by establishing appropriate substructural filters in the virtual screening stage. Amide derivatives of 8 and 12 preserved the inhibitory activity of parent compound 3, which provided a reasonable starting point for further structure-activity-relationship (SAR) studies on related compounds.
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Watanabe T. et al. Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 19. pp. 5807-5810.
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Watanabe T., UMEZAWA Y., Takahashi Y., AKAMATSU Y. Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 19. pp. 5807-5810.
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TY - JOUR
DO - 10.1016/j.bmcl.2010.07.131
UR - https://doi.org/10.1016/j.bmcl.2010.07.131
TI - Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Watanabe, Takumi
AU - UMEZAWA, YOJI
AU - Takahashi, Yoshikazu
AU - AKAMATSU, Yuzuru
PY - 2010
DA - 2010/10/01
PB - Elsevier
SP - 5807-5810
IS - 19
VL - 20
PMID - 20728352
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2010_Watanabe,
author = {Takumi Watanabe and YOJI UMEZAWA and Yoshikazu Takahashi and Yuzuru AKAMATSU},
title = {Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2010},
volume = {20},
publisher = {Elsevier},
month = {oct},
url = {https://doi.org/10.1016/j.bmcl.2010.07.131},
number = {19},
pages = {5807--5810},
doi = {10.1016/j.bmcl.2010.07.131}
}
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Watanabe, Takumi, et al. “Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 19, Oct. 2010, pp. 5807-5810. https://doi.org/10.1016/j.bmcl.2010.07.131.