Roberta Solidoro, Morena Miciaccia, Carmela Bonaccorso, Cosimo Gianluca Fortuna, Domenico Armenise, Antonella Centonze, Savina Ferorelli, Paola Vitale, Pryscila Rodrigues, Renilda Guimarães, Alana de Oliveira, Mariana da Paz, Luciana Rangel, Plínio Cunha Sathler, Angela Altomare, Maria Grazia Perrone, Antonio Scilimati
Cyclooxygenase enzymes have distinct roles in cardiovascular, neurological, and neurodegenerative disease. They are differently expressed in different type of cancers. Specific and selective COXs inhibitors are needed to be used alone or in combo-therapies. Fully understand the differences at the catalytic site of the two cyclooxygenase (COX) isoforms is still opened to investigation. Thus, two series of novel compounds were designed and synthesized in fair to good yields using the highly selective COX-1 inhibitor mofezolac as the lead compound to explore a COX-1 zone formed by the polar residues Q192, S353, H90 and Y355, as well as hydrophobic amino acids I523, F518 and L352...
January 10, 2024: European Journal of Medicinal Chemistry