Hepatitis C NS5B polymerase inhibitors: Functional equivalents for the benzothiadiazine moiety

• Published in: Bioorganic & medicinal chemistry letters Vol. 21; no. 6; pp. 1876 - 1879
• Main Authors: Hutchinson, Douglas K., Flentge, Charles A., Donner, Pamela L., Wagner, Rolf, Maring, Clarence J., Kati, Warren M., Liu, Yaya, Masse, Sherie V., Middleton, Tim, Mo, Hongmei, Montgomery, Debra, Jiang, Wen W., Koev, Gennadiy, Beno, David W.A., Stewart, Kent D., Stoll, Vincent S., Molla, Akhteruzzaman, Kempf, Dale J.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.03.2011; Elsevier
• Subjects: Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral agents; Benzothiadiazine; Benzothiadiazines - chemistry; Benzothiadiazines - pharmacology; Bioisosteres; Biological and medical sciences; chemistry; enzyme activity; Hepacivirus - enzymology; Hepacivirus - physiology; Hepatitis C; Medical sciences; NS5B polymerase inhibitors; Pharmacology. Drug treatments; Protease Inhibitors - chemistry; Protease Inhibitors - pharmacology; quinoline; replicon; Viral Nonstructural Proteins - antagonists & inhibitors; Virus Replication; Benzothiadiazine; Bioisosteres; Hepatitis C; NS5B polymerase inhibitors; Sulfonamide; Enzyme; Transferases; Quinoline derivatives; Enzyme inhibitor; In vitro; Biological activity; RNA-directed RNA polymerase; Virus; Nucleotidyltransferases; Antiviral; Flaviviridae; Chemical synthesis; Hepatitis C virus; Hepacivirus
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2010.12.067

A series of quinoline derivatives was synthesized as potential bioisosteric replacements for the benzothiadiazine moiety of earlier Hepatitis C NS5B polymerase inhibitors. Several of these compounds exhibited potent activity in enzymatic and replicon assays.