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 A scale-up of the protocol was explored using an unpublished methodology for the synthesis of a dapsone-precursor, which proved to be very effective over a short time.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.
BROAD SPECTRUM ANTIVIRAL COMPOUNDS AND USES THEREOF
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Paragraph 0378-0380, (2017/03/21)
Disclosed herein, inter alia, are agents having antiviral activity and methods of use thereof.
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
SAR and lead optimization of an HIV-1 Vif-APOBEC3G axis inhibitor
Mohammed, Idrees,Parai, Maloy K.,Jiang, Xinpeng,Sharova, Natalia,Singh, Gatikrushna,Stevenson, Mario,Rana, Tariq M.
supporting information; experimental part, p. 465 - 469 (2012/09/22)
We describe structure-activity relationship and optimization studies of RN-18, an HIV-1 Vif-APOBEC3G axis inhibitor. Targeted modifications of RN-18 ring C, ring B, ring A, bridge A-B, and bridge B-C were performed to identify the crucial structural features, which generated new inhibitors with similar (4g and 4i) and improved (5, 8b, and 11) activities. Two potent water-soluble RN-18 analogues, 17 and 19, are also disclosed, and we describe the results of pharmacological studies with compound 19. The findings described here will be useful in the development of more potent Vif inhibitors and in the design of probes to identify the target protein of RN-18 and its analogues.
ANTHRAPYRIDONE COMPOUND OR SALT THEREOF, MAGENTA INK COMPOSITION CONTAINING THE ANTHRAPYRIDONE COMPOUND, AND COLORED BODY
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Page/Page column 18, (2010/11/04)
The present invention relates to a novel anthrapyridone compound represented by the following formula (1) or a salt thereof: [wherein, R1 represents a hydrogen atom, an alkyl group or the like, R2 represents a hydrogen atom or a methoxy group and R3 represents an unsubstituted or substituted C5-C12 alkyl group, an unsubstituted or substituted aryl group, or an unsubstituted or substituted heteroaryl group, respectively; and with regard to the substitution positions of -SO2R3 and -SO3H whose substitution position are not specified and the both of which the benzene ring has thereon, one of their substitution positions is the para-position and the other thereof is the ortho-position to the substitution position of the nitrogen atom by which said benzene ring is substituted], and the compound of the present invention or a salt thereof has a hue which possesses high vividness suitable for inkjet recording, and provides a magenta coloring matter having higher fastnesses on recorded matter and excellent storage stability.
Composition and synthesis of new reagents for inhibition of HIV replication
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Page/Page column 16; 27; 28, (2008/06/13)
The present invention provides compounds and compositions for inhibiting Vif and methods for treating viral infection, e.g., HIV infection.
Synthesis of some 2-substituted-thioxanthones
Moon, Jung-Kyen,Park, Jung-Won,Lee, Woo Song,Kang, Young-Jin,Chung, Hyun-A.,Shin, Mi-Seon,Yoon, Yong-Jin,Park, Ki Hun
, p. 793 - 798 (2007/10/03)
This paper presents the synthesis of 2-amino-, 2-acetamido- and 2- benzamidothioxanthones and their 10,10-dioxides.
