Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit cyclooxygenase-1 (COX-1) and COX-2 enzymes. The NLRP3 inflammasome is a multi-protein complex responsible for the processing of the proinflammatory cytokine interleukin-1β and is implicated in many inflammatory diseases. Here we show that several clinically approved and widely used NSAIDs of the fenamate class are effective and selective in...

In a previous work the involvement of a fenamate-sensitive Ca(2+)-activated nonselective cation channel (NSCC) in free radical-induced rat liver cell necrosis was demonstrated (5). Therefore, we studied the effect of radical oxygen species and oxidizing agents on the gating behavior of a NSCC in a liver-derived epithelial cell line (HTC). Single-channel currents were recorded in HTC cells by th...

the uses of non-steroidal anti-inflammatory drugs (nsaids) are limited by a variety of side effects. so research on preparing new analgesic agents is important. according to some reports about the analgesic activity of hydrazide and hydrazine derivatives a new series of these compounds were synthesized in order to obtain new analgesic compounds. the final compounds 10a-10e and 15a-15d were prep...

PURPOSE The corneal epithelium provides a barrier between the external environment and the cornea. It also serves as an ion transporting epithelium. Because of its proximity with the external environment, the corneal epithelium is frequently injured through physical or chemical insult. The purpose of this study was to determine whether corneal epithelial cell whole-cell currents change during c...

Simon, Felipe, Diego Varela, Ana Luisa Eguiguren, Laı́n F. Dı́az, Francisco Sala, and Andrés Stutzin. Hydroxyl radical activation of a Ca -sensitive nonselective cation channel involved in epithelial cell necrosis. Am J Physiol Cell Physiol 287: C963–C970, 2004. First published May 26, 2004; 10.1152/ajpcell.00041.2004.—In a previous work the involvement of a fenamate-sensitive Ca activated nonsel...

VEGFR-2 is a critical target for the treatment of solid tumors. This work represents synthetic approaches to new class fenamate-based derivatives with essential pharmacophoric properties comparable inhibitors. The reaction tolfenamic acid hydrazide substituted phenacyl bromide, and phenylisothiocynate produced novel (TA) (compounds 4 5). molecules were validated using spectroscopic techniques s...