1052703-81-7Relevant articles and documents
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase
Kim, Sun Hee,Tran, Martin T.,Ruebsam, Frank,Xiang, Alan X.,Ayida, Benjamin,McGuire, Helen,Ellis, David,Blazel, Julie,Tran, Chinh V.,Murphy, Douglas E.,Webber, Stephen E.,Zhou, Yuefen,Shah, Amit M.,Tsan, Mei,Showalter, Richard E.,Patel, Rupal,Gobbi, Alberto,LeBrun, Laurie A.,Bartkowski, Darian M.,Nolan, Thomas G.,Norris, Daniel A.,Sergeeva, Maria V.,Kirkovsky, Leo,Zhao, Qiang,Han, Qing,Kissinger, Charles R.
scheme or table, p. 4181 - 4185 (2009/04/16)
A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of potent NS
A highly efficient, asymmetric synthesis of benzothiadiazine-substituted tetramic acids: Potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase
Fitch, Duke M.,Evans, Karen A.,Chai, Deping,Duffy, Kevin J.
, p. 5521 - 5524 (2007/10/03)
(Chemical Equation Presented) An efficient two-pot, asymmetric synthesis of benzothiadiazine-substituted tetramic acids is reported. Starting from commercially available α-amino acids or esters, reductive amination followed by a novel one-pot amide bond formation/Dieckmann cyclization provided the desired products in high yield and optical purity. An analogous solid-phase approach to the same targets is also presented. These compounds were found to be potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
