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Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Sep 15; Vol. 18 (18), pp. 5002-5. Date of Electronic Publication: 2008 Aug 09. - Publication Year :
- 2008
-
Abstract
- Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Among these, compound 4c displayed potent inhibitory activities in biochemical and replicon assays (IC(50) (1b) <10 nM; EC(50) (1b)=34 nM) as well as good stability towards human liver microsomes (HLM t(1/2) =59 min).
- Subjects :
- Antiviral Agents chemistry
Combinatorial Chemistry Techniques
Crystallography, X-Ray
Drug Design
Humans
Molecular Structure
Pyridazines chemistry
Structure-Activity Relationship
Antiviral Agents chemical synthesis
Antiviral Agents pharmacology
Hepacivirus drug effects
Microsomes, Liver drug effects
Pyridazines chemical synthesis
Pyridazines pharmacology
Viral Nonstructural Proteins antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18722768
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.08.017