Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery

Abstract

The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon).
 Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

Anti-Inflammatory Activity of Clove (Syzygium aromaticum) Oil Extract Against Chronic Inflammation in Rat

“…The suppression of fibroblasts, neutrophil infiltration, and exudation are signs of anti-inflammatory drug effectiveness in chronic inflammatory conditions (Ibrahim et al, 2016;Zhao et al, 2021). Our results about piroxicam were similar to the results of (Al-Khedairy, 2012;Abdulhadi et al, 2013). They reported that Non-steroidal anti-inflammatory medications (NSAIDs), such as piroxicam, reduce the size of granulomas by preventing granulocyte infiltration, delaying the production of collagen fibers, and suppressing mucopolysaccharides.…”