Design, synthesis, and biological evaluation of thiazoles targeting flavivirus envelope proteins.
Basic Information
ID: ALA1765083
Journal: J Med Chem
Title: Design, synthesis, and biological evaluation of thiazoles targeting flavivirus envelope proteins.
Authors: Mayhoub AS, Khaliq M, Kuhn RJ, Cushman M.
Abstract: A series of third-generation analogues of methyl 4-(dibromomethyl)-2-(4-chlorophenyl)thiazole-5-carboxylate (1), which had the most potent antiviral activity among the first- and second-generation compounds, have been synthesized and tested against yellow fever virus using a cell-based assay. The compounds were designed with the objectives of improving metabolic stability, therapeutic index, and antiviral potency. The biological effects of C4 and C5 substitution were examined. The methylthio ester and the dihydroxypropylamide analogues had the best antiviral potencies and improved therapeutic indices and metabolic stabilities relative to the parent compound 1.
CiteXplore: 21355607
DOI: 10.1021/jm1013538
Patent ID: ┄