A new series of HCV inhibitors based on a 2-(thieno[2,3]pyridin-2-yl)-1,3,4-oxadiazole scaffold
A new series of HCV inhibitors based on a 2-(thieno[2,3- b ]pyridin-2-yl)-1,3,4-oxadiazole scaffold was developed. Detailed SAR investigations revealed the HCV inhibitory activity was sensitive to the size of C5, the C6-fused ring, and the size and flexibility of C5′ cycloalkane, which led to the id...
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Veröffentlicht in: | RSC advances 2016-01, Vol.6 (46), p.4277-4286 |
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Hauptverfasser: | , , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | A new series of HCV inhibitors based on a 2-(thieno[2,3-
b
]pyridin-2-yl)-1,3,4-oxadiazole scaffold was developed. Detailed SAR investigations revealed the HCV inhibitory activity was sensitive to the size of C5, the C6-fused ring, and the size and flexibility of C5′ cycloalkane, which led to the identification of several compounds with potent inhibitory activity against HCV genotype 1b replicon. The most potent compound
10d
showed ∼100-fold improvement in potency compared with compound
1
, with an EC
50
of 0.039 μM, but without obvious cytotoxicity
in vitro
.
A new series of HCV inhibitors based on a 2-(thieno[2,3-
b
]pyridin-2-yl)-1,3,4-oxadiazole scaffold was developed. |
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ISSN: | 2046-2069 2046-2069 |
DOI: | 10.1039/c6ra01179a |