Identification of a unique nsaid, fluoro-loxoprofen with gastroprotective activity

Structure–activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity

“…In fact, we recently reported that screening for NSAIDs with lower membrane permeabilizing activity resulted in the identification of an interesting new NSAID, fluoro-loxoprofen, which has much lower membrane permeabilizing and gastric ulcerogenic activities compared with clinically used NSAIDs. [27][28][29][30][31] These results suggest that NSAIDs with lower membrane permeabilizing activity could be therapeutically beneficial. Thus, it is important to understand how the membrane permeabilizing properties of NSAIDs are affected by their structure-activity relationship.…”

Analgesic activity of new 8-methoxy-1,3-dimethyl-2,6-dioxo-purin-7-yl derivatives with carboxylic, ester or amide moieties

“…Efforts to discover new anti-inflammatory analgesic agents concentrated on synthesis structural analogs of active compounds with limited hepatotoxicity, nefrotoxicity, and propensity to include gastric or intestinal ulceration [3,4]. The main objective in current pain research is to develop improved non-opioid analgesics with better efficacy and safety.…”

Synthesis and characterisation of glucosamine–NSAID bioconjugates

“…Thus masking the carboxylic acid functionality of these drugs as pro-drugs can reduce this topical irritation. Various synthetic strategies to reduce gastric ulceration caused by NSAIDs have been investigated, including substitution of aromatic protons for fluorine, 10 synthesis of ester or amide pro-drugs 11 and conjugation of NSAIDs to carbohydrates, 12 gastro-protective drugs 2c and acetaminophen. 13 Galanakis et al 14 showed that amidation of indomethacin and diclofenac with L-cysteine ethyl ester resulted in pro-drugs with enhanced anti-inflammatory properties in addition to anti-oxidant properties.…”