20904-30-7Relevant articles and documents
Cerium catalyst promoted C-S cross-coupling: Synthesis of thioethers, dapsone and RN-18 precursors
Tavares Junior, José M. Da C.,Da Silva, Caren D. G.,Dos Santos, Beatriz F.,Souza, Nicole S.,De Oliveira, Aline R.,Kupfer, Vicente L.,Rinaldi, Andrelson W.,Domingues, Nelson L. C.
supporting information, p. 10103 - 10108 (2019/12/23)
In this work, we present a novel, efficient and green methodology for the synthesis of thioethers by the C-S cross-coupling reaction with the assistance of [Ce(l-Pro)2]2Ox as a heterogeneous catalyst in good to excellent yields. A scale-up of the protocol was explored using an unpublished methodology for the synthesis of a dapsone-precursor, which proved to be very effective over a short time. The catalyst [Ce(l-Pro)2]2Ox was recovered and it was shown to be effective for five more reaction cycles.
Novel dengue virus NS2B/NS3 protease inhibitors
Wu, Hongmei,Bock, Stefanie,Snitko, Mariya,Berger, Thilo,Weidner, Thomas,Holloway, Steven,Kanitz, Manuel,Diederich, Wibke E.,Steuber, Holger,Walter, Christof,Hofmann, Daniela,Wei?brich, Benedikt,Spannaus, Ralf,Acosta, Eliana G.,Bartenschlager, Ralf,Engels, Bernd,Schirmeister, Tanja,Bodem, Jochen
supporting information, p. 1100 - 1109 (2015/03/05)
Dengue fever is a severe, widespread, and neglected disease with more than 2 million diagnosed infections per year. The dengue virus NS2B/NS3 protease (PR) represents a prime target for rational drug design. At the moment, there are no clinical PR inhibitors (PIs) available. We have identified diaryl (thio)ethers as candidates for a novel class of PIs. Here, we report the selective and noncompetitive inhibition of the serotype 2 and 3 dengue virus PR in vitro and in cells by benzothiazole derivatives exhibiting 50% inhibitory concentrations (IC50s) in the low-micromolar range. Inhibition of replication of DENV serotypes 1 to 3 was specific, since all substances influenced neither hepatitis C virus (HCV) nor HIV-1 replication. Molecular docking suggests binding at a specific allosteric binding site. In addition to the in vitro assays, a cell-based PR assay was developed to test these substances in a replication-independent way. The new compounds inhibited the DENV PR with IC50s in the low-micromolar or submicromolar range in cells. Furthermore, these novel PIs inhibit viral replication at submicromolar concentrations.
Synthesis and structure-activity relationship studies of hiv-1 virion infectivity factor (vif) inhibitors that block viral replication
Ali, Akbar,Wang, Jinhua,Nathans, Robin S.,Cao, Hong,Sharova, Natalia,Stevenson, Mario,Rana, Tariq M.
, p. 1217 - 1229 (2012/07/17)
The human immunodeficiency virus1 (HIV-1) virion infectivity factor (Vif) protein, essential for in vivo viral replication, protects the virus from innate antiviral cellular factor apolipoproteinB mRNA-editing, enzyme-catalytic, polypeptide-like3G (APOBEC
