Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors

Title
Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors
Authors
배일학김희선유영수추지연최원우선민경이승기금교창장승기김병문
Keywords
HCV; NS5A inhibitor; Benzidine; Diaminofluorene; Structureeactivity relationship
Issue Date
2015-08
Publisher
European journal of medicinal chemistry
Citation
VOL 101, 163-178
Abstract
Our study describes the discovery of a series of highly potent hepatitis C virus (HCV) NS5A inhibitors based on symmetrical prolinamide derivatives of benzidine and diaminofluorene. Through modification of benzidine, l-proline, and diaminofluorene derivatives, we developed novel inhibitor structures, which allowed us to establish a library of potent HCV NS5A inhibitors. After optimizing the benzidine prolinamide backbone, we identified inhibitors embedding meta-substituted benzidine core structures that exhibited the most potent anti-HCV activities. Furthermore, through a battery of studies including hERG ligand binding assay, CYP450 binding assay, rat plasma stability test, human liver microsomal stability test, and pharmacokinetic studies, the identified compounds 24, 26, 27, 42, and 43 are found to be nontoxic, and are expected to be effective therapeutic anti-HCV agents
URI
http://pubs.kist.re.kr/handle/201004/50079
ISSN
02235234
Appears in Collections:
KIST Publication > Article
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