Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis
Hiroshi Takeshita
1
,
Jun WATANABE
1
,
Yoichi Kimura
2
,
Katsuhiro Kawakami
1
,
Hisashi Takahashi
1
,
Makoto TAKEMURA
1
,
Akihiro Kitamura
3
,
Kazuhiko SOMEYA
4
,
Ryohei Nakajima
5
Publication type: Journal Article
Publication date: 2010-07-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
20605446
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
We have discovered novel pyridobenzimidazole derivatives, which exhibit antifungal activity by the inhibition of β-1,6-glucan synthesis. Based on the HTS hit compound 1a , an inhibitor of β-1,6-glucan synthesis, we synthesized novel pyridobenzimidazole derivatives and evaluated their antifungal activity. Among the compounds synthesized, we identified the potent compound 15e , which exhibits excellent activity superior to fluconazole against both Candida glabrata and Candida krusei . From the SAR study, we revealed essential moieties for antifungal activity.
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64
Total citations:
64
Citations from 2025:
1
(1.56%)
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GOST
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Takeshita H. et al. Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 13. pp. 3893-3896.
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Takeshita H., WATANABE J., Kimura Y., Kawakami K., Takahashi H., TAKEMURA M., Kitamura A., SOMEYA K., Nakajima R. Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 13. pp. 3893-3896.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2010.05.024
UR - https://doi.org/10.1016/j.bmcl.2010.05.024
TI - Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Takeshita, Hiroshi
AU - WATANABE, Jun
AU - Kimura, Yoichi
AU - Kawakami, Katsuhiro
AU - Takahashi, Hisashi
AU - TAKEMURA, Makoto
AU - Kitamura, Akihiro
AU - SOMEYA, Kazuhiko
AU - Nakajima, Ryohei
PY - 2010
DA - 2010/07/01
PB - Elsevier
SP - 3893-3896
IS - 13
VL - 20
PMID - 20605446
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
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@article{2010_Takeshita,
author = {Hiroshi Takeshita and Jun WATANABE and Yoichi Kimura and Katsuhiro Kawakami and Hisashi Takahashi and Makoto TAKEMURA and Akihiro Kitamura and Kazuhiko SOMEYA and Ryohei Nakajima},
title = {Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2010},
volume = {20},
publisher = {Elsevier},
month = {jul},
url = {https://doi.org/10.1016/j.bmcl.2010.05.024},
number = {13},
pages = {3893--3896},
doi = {10.1016/j.bmcl.2010.05.024}
}
Cite this
MLA
Copy
Takeshita, Hiroshi, et al. “Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of β-1,6-glucan synthesis.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 13, Jul. 2010, pp. 3893-3896. https://doi.org/10.1016/j.bmcl.2010.05.024.