期刊
CHEMISTRY & BIODIVERSITY
卷 19, 期 2, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.202100602
关键词
imidazolinone with 5-arylidene and 2-substituted mercapto group; anti-HCV compounds; direct-acting; antiviral activity
资金
- National Key R&D Program of China [2018YFA0507603]
- National Natural Science Foundation of China [91740120, 21572173]
- National Grand Program on Key Infectious Disease of China [2017ZX10201301-006]
- National Outstanding Youth Foundation of China [81025008]
- major projects of technological innovation of Hubei Province [2016ACA150, 2016CFA062]
- Key R&D Program of Hubei Province [2020BCB020]
- Hubei Province's Outstanding Medical Academic Leader Program [523-276003]
- Innovative group project of Hubei Health Committee [WJ2021C002]
- Foundational Research Funds for the Central University of China
- Open Research Fund Program of the State Key Laboratory of Virology of China [2018KF008]
Six novel imidazolinone derivatives were synthesized, and compound 4b, containing 5-para-methoxy-phenylidene and 2-thioalkylation terminal substitution, exhibited the strongest anti-HCV activity and the lowest cytotoxicity. The selectivity index (SI=CC50/IC50) of 4b was determined to be 36, indicating its high selectivity towards HCV.
Here six novel imidazolinone derivatives have been synthesized and the compound 4b containing 5-para-methoxy-phenylidene and 2-thioalkylation terminal substitution with 3'-cyano-2',6'-dimethylphenyl showed the best anti-HCV activity and the lowest cytotoxicity. Selectivity index (SI=CC50/IC50) for the 4b was determined as 36, indicating that compound 4b was highly selective towards HCV.
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