Discovery of Pyrano[3,4-b]indoles as Potent and Selective HCV NS5B Polymerase Inhibitors

A novel series of HCV NS5B RNA-dependent RNA polymerase inhibitors containing a pyrano[3,4-b]indole scaffold is described leading to the discovery of compound 16, a highly potent and selective inhibitor that is active in the replicon system.

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Veröffentlicht in:	Journal of medicinal chemistry 2004-12, Vol.47 (26), p.6603-6608
Hauptverfasser:	Gopalsamy, Ariamala, Lim, Kitae, Ciszewski, Gregory, Park, Kaapjoo, Ellingboe, John W, Bloom, Jonathan, Insaf, Shabana, Upeslacis, Janis, Mansour, Tarek S, Krishnamurthy, Girija, Damarla, Murthy, Pyatski, Yelena, Ho, Douglas, Howe, Anita Y. M, Orlowski, Mark, Feld, Boris, O'Connell, John
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Biological and medical sciences Crystallography, X-Ray DNA-Directed RNA Polymerases - antagonists & inhibitors DNA-Directed RNA Polymerases - chemistry Hepacivirus - enzymology Hepatitis C virus Indoles - chemical synthesis Indoles - chemistry Medical sciences Pharmacology. Drug treatments Pyrans - chemical synthesis Pyrans - chemistry Stereoisomerism Structure-Activity Relationship Viral Nonstructural Proteins - antagonists & inhibitors Viral Nonstructural Proteins - chemistry
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Beschreibung
Zusammenfassung:	A novel series of HCV NS5B RNA-dependent RNA polymerase inhibitors containing a pyrano[3,4-b]indole scaffold is described leading to the discovery of compound 16, a highly potent and selective inhibitor that is active in the replicon system.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm0401255