92696-68-9Relevant academic research and scientific papers
Design and synthesis of 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran derivatives as non-nucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase
Gopalsamy, Ariamala,Aplasca, Alexis,Ciszewski, Gregory,Park, Kaapjoo,Ellingboe, John W.,Orlowski, Mark,Feld, Boris,Howe, Anita Y.M.
, p. 457 - 460 (2006)
A novel class of HCV NS5B RNA dependent RNA polymerase inhibitors containing 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H- pyrano[3,4-b]benzofuran scaffolds were designed and synthesized. Optimization of the alkyl substituent in the pyran ring showed preference for an n-propyl group, while 5,8-disubstitution pattern is preferred for the aromatic region. Analog 19 displayed potent activity with an IC50 of 50 nM against HCV NS5B enzyme and was selective over a panel of polymerases.
NON-SYSTEMIC TGR5 AGONISTS
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Page/Page column 93, (2013/07/05)
Compounds of structure (I), or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
