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Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Feb 15; Vol. 18 (4), pp. 1413-8. Date of Electronic Publication: 2008 Jan 08. - Publication Year :
- 2008
-
Abstract
- 5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as inhibitors of genotype 1 HCV NS5B polymerase. The synthesis, structure-activity relationships (SAR), metabolic stability, and structure-based design approach for this new class of compounds are discussed.
- Subjects :
- Benzothiadiazines metabolism
Crystallography, X-Ray
Drug Design
Drug Stability
Enzyme Inhibitors metabolism
Humans
Hydrogen Bonding
Inhibitory Concentration 50
Microsomes, Liver metabolism
Models, Molecular
Pyridazines metabolism
RNA-Dependent RNA Polymerase antagonists & inhibitors
RNA-Dependent RNA Polymerase metabolism
Structure-Activity Relationship
Viral Nonstructural Proteins metabolism
Benzothiadiazines chemistry
Benzothiadiazines pharmacology
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Pyridazines chemistry
Pyridazines pharmacology
Viral Nonstructural Proteins antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18242088
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.01.007