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Full-Text Articles in Chemistry
Synthesis Of A Small Molecule Nitrosocysteine Inhibitor To Reduce The Activity Of Caspase-1, Catherine A. Shamblen, Caitlin E. Karver
Synthesis Of A Small Molecule Nitrosocysteine Inhibitor To Reduce The Activity Of Caspase-1, Catherine A. Shamblen, Caitlin E. Karver
DePaul Discoveries
Caspase-1 is an enzyme that is overactive in autoimmune and autoinflammatory diseases cleaving pro-interleukin-1β to the cytokine interleukin-1β (IL-1β), which leads to inflammatory symptoms. The inhibition of caspase-1 will cause a decrease in the concentration of interleukin-1β (IL-1β), resulting in the reduction of inflammatory symptoms. Recent research has revealed that the appending of a nitric oxide (NO) or nitroxyl (HNO) donating group to non-steroidal anti-inflammatory drugs (NSAIDs) reduced, or avoided, the side effects caused by currently available treatments. A small molecule based on a known caspase-1 inhibitor with a nitrosocysteine appended on was synthesized to look at the effect of …
Serendipitous Discovery Of A New Method For The Catalytic Synthesis Of Indole-Fused Benzazepanes, Edward Gluzman, Paul A. Vadola
Serendipitous Discovery Of A New Method For The Catalytic Synthesis Of Indole-Fused Benzazepanes, Edward Gluzman, Paul A. Vadola
DePaul Discoveries
We report here on our investigations into the application of 1,5-hydride transfer cyclization mechanisms to the synthesis of 2,3-disubstituted benzofurans and indoles. We found that PtI4 in MeCN at 120 ºC was indeed capable of activating the alkyne, however, the expected 2,3-disubstituted indole product was not observed. Instead we isolated an indolyl-3-benzazepane via an unexpected intramolecular Steven’s rearrangement/ring expansion. While this transformation has been previously reported our method may prove to have increased substrate scope and more practical reaction conditions. Further studies are underway to optimize the reaction conditions and to fully explore the scope and mechanism of the …