774575-92-7Relevant academic research and scientific papers
Hepatoselectivity of statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors
Park, William K.C.,Kennedy, Robert M.,Larsen, Scott D.,Miller, Steve,Roth, Bruce D.,Song, Yuntao,Steinbaugh, Bruce A.,Sun, Kevin,Tait, Bradley D.,Kowala, Mark C.,Trivedi, Bharat K.,Auerbach, Bruce,Askew, Valerie,Dillon, Lisa,Hanselman, Jeffrey C.,Lin, Zhiwu,Lu, Gina H.,Robertson, Andrew,Sekerke, Catherine
, p. 1151 - 1156 (2008/09/19)
4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The compounds were prepared via a [3 + 2] cycloaddition of a Muenchnone with a sulfonamide-substituted alkyne. We identified compounds with greater selectivity for hepatocytes compared to L6-myocytes than rosuvastatin and atorvastatin. There was an inverse correlation of myocyte potencies and C log P values. A number of analogs were effective at reducing cholesterol in acute and chronic in vivo models but they lacked sufficient chronic in vivo activity to warrant further development.
NOVEL PYRROLE-BASED HMG-COA REDUCTASE INHIBITORS
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Page/Page column 93, (2010/02/10)
HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Method of making and methods of using the compounds are also provided.
Sulfur dioxide mediated one-pot, three- and four-component syntheses of polyfunctional sulfonamides and sulfonic esters: Study of the stereoselectivity of the ene reaction of sulfur dioxide
Bouchez, Laure C.,Dubbaka, Srinivas Reddy,Turks, Maris,Vogel, Pierre
, p. 6413 - 6418 (2007/10/03)
The ene reaction of sulfur dioxide with enoxysilanes or with allylsilanes generates silyl sulfinates that can be brominated (Br2 or NBS) or chlorinated (NCS or Cl2) to produce the corresponding sulfonyl halides. They react with prima
Polyfunctional sulfonamides and sulfonates and process for preparing them
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Page 10; 12, (2008/06/13)
The present invention relates to a process for preparing sulfonyl halides comprising the steps of a) reacting an enoxymetal, allylsilane or allylstannane compound, preferably in the presence of a diene, with sulphur dioxide and b) adding a suitable halogen source to the metal sulfinate intermediate of step a). Furthermore, the present invention relates to new sulfonyl chlorides, bromides, and iodides, sulfonamides and sulfonates. In addition, the present invention teaches the use of the new multifunctional sulfonamides and sulfonates for the preparation of a medicament, bacteriocides, fungicides, pesticides, and herbicides as well as the use of sulfonyl chlorides for the preparation of sulfonamides and sulfonates.
