124010-13-5Relevant articles and documents
MLKL INHIBITORS
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, (2018/09/26)
Purine derivatives that inhibit cellular necroptosis and/or human MLKL, pharmaceutical compositions thereof, and methods of treating an MLKL-mediated disorder with an effective amount of the compound or composition. Said MLKL-mediated disorder is pathology associated necroptosis, including ischemia-reperfusion damage, neurodegeneration, and inflammatory diseases such as acute pancreatitis, multiple sclerosis, inflammatory bowel disease, and allergic colitis.
Geographic variability and anti-staphylococcal activity of the chrysophaentins and their synthetic fragments
Keffer, Jessica L.,Hammill, Jared T.,Lloyd, John R.,Plaza, Alberto,Wipf, Peter,Bewley, Carole A.
, p. 1103 - 1125 (2012/08/14)
Drug-resistant Staphylococcus aureus is a continuing public health concern, both in the hospital and community settings. Antibacterial compounds that possess novel structural scaffolds and are effective against multiple S. aureus strains, including current drug-resistant ones, are needed. Previously, we have described the chrysophaentins, a family of bisdiarylbutene macrocycles from the chrysophyte alga Chrysophaeum taylori that inhibit the growth of S. aureus and methicillin-resistant S. aureus (MRSA). In this study we have analyzed the geographic variability of chrysophaentin production in C. taylori located at different sites on the island of St. John, U.S. Virgin Islands, and identified two new linear chrysophaentin analogs, E2 and E3. In addition, we have expanded the structure activity relationship through synthesis of fragments comprising conserved portions of the chrysophaentins, and determined the antimicrobial activity of natural chrysophaentins and their synthetic analogs against five diverse S. aureus strains. We find that the chrysophaentins show similar activity against all S. aureus strains, regardless of their drug sensitivity profiles. The synthetic chrysophaentin fragments indeed mimic the natural compounds in their spectrum of antibacterial activity, and therefore represent logical starting points for future medicinal chemistry studies of the natural products and their analogs.
Ethyl(or methyl) 4-acetoxy(or propionyloxy)-5,6,7 or 8-di(or tri-)substituted-2-naphthoates
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, (2008/06/13)
Novel antiviral ring-substituted ethyl or methyl 4-acetoxy (or propionyloxy)-2-naphthoates are provided.
AN EFFICIENT ROUTE TO 3-CHLOROJUGLONES
Bloomer, James L.,Gazzillo, Joseph A.
, p. 1201 - 1204 (2007/10/02)
The novel 4-chloro-2,5-dimethoxybenzaldehyde 1 has been prepared and converted in only three steps to 5-acetoxy-7-carboethoxy-3-chloro-1,4-naphthaquinone 4.Subsequent Diels-Alder reaction affords a tetracyclic enol ether 9 in a regiospecific manner.