Koszyk Francis

TL;DR: A series of heteroaryl modified 1,2-diarylimidazoles has been synthesized and found to be potent and highly selective (1000−9000-fold) inhibitors of the human COX-2 as discussed by the authors.

TL;DR: A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of 1 (SC-102) bound to p38 enzyme, and a compound identified from this series was efficacious in an animal model of rheumatic disease.

TL;DR: The substituted 2-trifluoromethyl-2H-benzopyran-3-carboxylic acids as a novel series of potent and selective cyclooxygenase-2 (COX-2) inhibitors is reported.

TL;DR: The subject of as discussed by the authors concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders, and the compounds of particular interest are benzopyrans and their analogs defined by formula (1).

TL;DR: A series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1beta stimulated synovial fibroblasts and identified as the most potent inhibitors with improved cellular activity.