Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): Central amino acid linker and right-hand-side SAR studies

In this part 2, new indole 5-carboxamide Thumb Pocket 1 inhibitors of HCV NS5B polymerase are described. Structure–activity relationships (SAR) were explored at the central amino acid linker position and the right-hand-side of the molecule in an attempt to identify molecules with a balanced overall...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-06, Vol.21 (12), p.3664-3670
Hauptverfasser:	Beaulieu, Pierre L., Chabot, Catherine, Duan, Jianmin, Garneau, Michel, Gillard, James, Jolicoeur, Eric, Poirier, Martin, Poupart, Marc-André, Stammers, Timothy A., Kukolj, George, Tsantrizos, Youla S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation Amino Acid Sequence amino acids Amino Acids - chemical synthesis Amino Acids - chemistry Amino Acids - pharmacology Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral Antiviral agents Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Caco-2 Cells HCV Hepacivirus - drug effects Hepacivirus - enzymology Hepacivirus - genetics Hepatitis C virus Humans Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Inhibitor Inhibitory Concentration 50 Medical sciences Molecular Sequence Data Molecular Structure NS5B polymerase Pharmacology. Drug treatments physicochemical properties Rats SAR Solubility Structure-Activity Relationship structure-activity relationships Viral Nonstructural Proteins - antagonists & inhibitors Viral Nonstructural Proteins - genetics
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Beschreibung
Zusammenfassung:	In this part 2, new indole 5-carboxamide Thumb Pocket 1 inhibitors of HCV NS5B polymerase are described. Structure–activity relationships (SAR) were explored at the central amino acid linker position and the right-hand-side of the molecule in an attempt to identify molecules with a balanced overall profile of potency (EC 50
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.04.082