The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase.
Bioorg Med Chem Lett
; 14(12): 3257-61, 2004 Jun 21.
Article
in En
| MEDLINE
| ID: mdl-15149686
ABSTRACT
Screening of the in-house sample collection for compounds with HCV NS5B RNA dependent RNA polymerase inhibition led to the identification of a new lead. Afterwards, we discovered that the screening lead, rather than containing the expected structure 1, was comprised of roughly a 11 mixture of meconic acid 2 and its monoethyl ester 3, with all inhibitory potency residing with 3. We propose that this compound shares critical common features for activity with alpha,gamma-diketoacids inhibitors previously discovered by our group. SAR around this molecule will be presented to provide an improved basis for structure-based ligand design.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Pyrones
/
RNA-Dependent RNA Polymerase
/
RNA, Viral
/
Viral Nonstructural Proteins
/
Hepacivirus
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2004
Document type:
Article
Affiliation country:
Italy