Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (10), p.2481-2486
2005
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Details
- Autor(en) / Beteiligte
- Titel
- Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (10), p.2481-2486
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2005
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- [Display omitted] A novel series of nonnucleoside HCV NS5B polymerase inhibitors were prepared from (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid, a high throughput screening lead. SAR studies combined with structure based drug design focusing on the southern heterobiaryl region of the template led to the synthesis of several potent and orally bioavailable lead compounds. X-ray crystallography studies were also performed to understand the interaction of these inhibitors with HCV NS5B polymerase.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2005.03.066Titel-ID: cdi_crossref_primary_10_1016_j_bmcl_2005_03_066
- Format
- –
- Schlagworte
- Acrylates - chemistry, Acrylates - pharmacokinetics, Acrylates - pharmacology, Antibiotics. Antiinfectious agents. Antiparasitic agents, Antiviral agents, Biological and medical sciences, Biological Availability, Crystallography, X-Ray, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacokinetics, Enzyme Inhibitors - pharmacology, Furans - chemistry, Furans - pharmacokinetics, Furans - pharmacology, HCV Polymerase, Inhibitors, Medical sciences, Pharmacology. Drug treatments, Structure-Activity Relationship, Viral Nonstructural Proteins - antagonists & inhibitors