2527-62-0Relevant academic research and scientific papers
Preparation of benzisothiazolones from 2-bromobenzamides and sulfur under copper catalysis conditions
Krasikova,Katkevics
, p. 1684 - 1690 (2013/07/04)
A convenient two-stage method has been developed for preparing benz[d]isothiazol-3(2H)-ones from 2-bromobenzamides and sulfur in a one-pot process under copper catalysis conditions. The method is suitable for the synthesis of N-aryl-, benzyl-, and alkyl-substituted benzisothiazolones. The yields of the benzisothiazolones depend on the nature of the starting amide and can reach 91%.
Crucial role of selenium in the virucidal activity of benzisoselenazol- 3(2h)-ones and related diselenides
Pietka-Ottlik, Magdalena,Potaczek, Piotr,Piasecki, Egbert,Mlochowski, Jacek
experimental part, p. 8214 - 8228 (2011/03/19)
Various N-substituted benzisoselenazol-3(2H)-ones and their non-seleniumcontaining analogues have been synthesized and tested against selected viruses (HHV-1, EMCV and VSV) to determine the extent to which selenium plays a role in antiviral activity. The data presented here show that the presence of selenium is crucial for the antiviral properties of benzisoselenazol-3(2H)-ones since their isostructural analogues having different groups but lacking selenium either did not show any antiviral activity or their activity was substantially lower. The open-chain analogues of benzisoselenazol- 3(2H)-ones-diselenides also exhibited high antiviral activity while selenides and disulfides were completely inactive towards model viruses.
Cu and Ag catalyzed oxidative arylthiation of terminal acetylenes
Henke, Adam,Srogl, Jiri
supporting information; experimental part, p. 6819 - 6821 (2010/10/20)
A mild Cu or Ag catalyzed oxidative arylthiation of terminal acetylenes is introduced. The process, featuring metal catalyzed C-H bond activation as a key step, leads to the formation of highly substituted mercaptoacetylenes under unprecedented neutral conditions.
A new class of anti-HIV-1 agents targeted toward the nucleocapsid protein NCp7: The 2,2'-dithiobisbenzamides
Domagala, John M.,Bader, John P.,Gogliotti, Rocco D.,Sanchez, Joseph P.,Stier, Michael A.,Song, Yuntao,Vara Prasad,Tummino, Peter J.,Scholten, Jeffrey,Harvey, Patricia,Holler, Tod,Gracheck, Steve,Hupe, Donald,Rice, William G.,Schultz, Robert
, p. 569 - 579 (2007/10/03)
As part of the National Cancer Institute's Drug Screening Program, a new class of antiretrovirals active against the human immunodeficiency virus HIV-1 has been identified, and the HIV-1 nucleocapsid protein NCp7 was proposed as the target of antiviral action. The 2,2'-dithiobis-[4'-(sulfamoyl)benzanilide] (3x) and the 2,2'-dithiobis(5-acetylamino)benzamide (10) represented the prototypic lead structures. A wide variety of 2,2'-dithiobisbenzamides were prepared and tested for anti-HIV-1 activity, cytotoxicity, and their ability to extrude zinc from the zinc fingers for NCp7. The structure-activity relationships demonstrated that the ability to extrude zinc from NCp7 resided in the 2,2'-dithiobisbenzamide core structure. The 3,3' and the 4,4' isomers were inactive. While many analogs based upon the core structure retained the zinc extrusion activity, the best overall anti-HIV-1 activity was only found in a narrow set of derivatives possessing carboxylic acid, carboxamide, or phenylsulfonamide functional groups. These functional groups were more important for reducing cytotoxicity than improving antiviral potency or activity vs NCp7. All of the compounds with antiviral activity also extruded zinc from NCp7. From this study several classes of low μM anti-HIV agents with simple chemical structures were identified as possible chemotherapeutic agents for the treatment of AIDS.
Antithrombotic agent
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, (2008/06/13)
Certain 2,2'-dithiobis-N-substituted or unsubstituted benzamides or derivatives thereof are useful as antithrombotic agents because of their ability to suppress aggregation of blood platelets.
STUDIES ON ORGANOPHOSPHORUS COMPOUNDS. THIATION OF 3,1-BENZOXATHIAN-4-ONES. NEW ROUTES TO 1,2-BENZISOTHIAZOLE-3(2H)-THIONES AND 3H-1,2-BENZODITHIOL-3-IMINES
El-Barbary, A. A.,Clausen, K.,Lawesson, S.-O.
, p. 3309 - 3316 (2007/10/02)
3,1-Benzoxathian-4-ones, 2, when heated with 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane-2,4-disulfide, 1, or with P4S10 give one or more of the following products: 3,1-benzoxathian-4-thione, 3, 1,3-benzodithian-4-one, 4, 1,3-benzodithian-4-thion
