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Full-Text Articles in Other Chemicals and Drugs
Greener Synthesis Of Pdi Ligands Using A Microwave Reactor, Gabrielle E. Leonhardt, Abbigale S. Holjes, Kyle A. Grice
Greener Synthesis Of Pdi Ligands Using A Microwave Reactor, Gabrielle E. Leonhardt, Abbigale S. Holjes, Kyle A. Grice
DePaul Discoveries
Two pyridinediimine (PDI) ligands were synthesized using green chemistry principles to minimize environmental impact and maintain synthetic efficiency. Previous syntheses require hazardous solvents and long reaction times. The reaction was carried out with a safer solvent, ethanol, and more rapidly using a CEM Discover microwave reactor. The PDI ligand was chosen for the scaffold for the aromatic core and support for different aniline derivatives. Comparative investigation of aniline electronics showed that 2,6-dimethylaniline was more successful than the electron-withdrawing electronics of 2,6-dichloroaniline. Synthesized complexes were characterized with proton nuclear magnetic resonance (NMR). The environmentally conscious microwave reaction produced effective and reproducible …
Synthesis Of Triaminopyrimidine Derivatives For Inhibition Of Inflammatory Caspases, Marianna C. Haddad, Caitlin Karver
Synthesis Of Triaminopyrimidine Derivatives For Inhibition Of Inflammatory Caspases, Marianna C. Haddad, Caitlin Karver
DePaul Discoveries
Caspases are cysteine-dependent aspartic proteases whose functions are connected to different mechanisms of cell death and inflammation. As caspase-1 plays a significant role in the immune response, its activity has been of interest as a target for inhibitor development as its inhibition will reduce the levels of pro-inflammatory cytokines in inflammatory diseases, thus minimizing the symptoms that arise and serving as a possible therapeutic approach. Prior work discovered a family of potent inhibitors of caspase-1 with a common triaminopyrimidine scaffold. To further explore structure-activity relationship profiles of potential inhibitors of caspase-1, two different syntheses were attempted to create two new …
Small Molecule Inhibitors Of Inflammatory Caspases-1, -4, And -5, Christopher D. Ahlers
Small Molecule Inhibitors Of Inflammatory Caspases-1, -4, And -5, Christopher D. Ahlers
DePaul Discoveries
Inflammatory caspases-1, -4, and -5 play critical roles in mediating the innate immune response to pathogen- and damage-associated molecular patterns. Caspase-1 produces the cytokine interleukin-1β (IL-1β), while caspases-4 and -5 activate the NOD-like receptor protein 3 inflammasome via the non-canonical pathway. Overactivation of these enzymes is associated with an increased risk for inflammatory diseases such as lupus, psoriasis, and rheumatoid arthritis. Small molecule inhibitors (SMIs) have been developed to attenuate the production of IL-1β, but unfavorable bioavailability and toxicity have provided an insurmountable barrier in clinical trials. This work is concerned with delivering an overview of current progress in the …