Synthesis and pharmacological characterization of benzenesulfonamides as dual species inhibitors of human and murine mPGES-1

Nonsteroidal Anti‐Inflammatory Therapy: A Journey Toward Safety

“…The screening of compound libraries has permitted the further identification of a wide variety of promising scaffolds to design potent and selective mPGES‐1 inhibitors, namely, (Z)‐5‐benzylidene‐2‐iminothiazolidin‐4‐one, aminothiazole, triazole, s‐triazine, benzenesulfonamide, trisubstituted urea, sulfonylhydrazide, carbazole benzamide, and pyrazolone . In some cases, in vivo experiments have demonstrated the potential effectiveness of these mPGES‐1 inhibitors to treat inflammatory conditions.…”

Recent Functionalizations of Primary Sulfonamides

“…[15][16][17][18][19] Sulfonamides have a wide range of medical applications due to their anti-inflammatory, [15][16][17] antibacterial, [18][19][20][21] antimicrobial, [22][23][24] anticancer, [25][26][27][28][29][30][31] antimalarial, 32 and antipsychotic activities. 33 They have been reported to be inhibitors of DNA double-strand break repair, 34 dual angiotensin II and endothelin A receptor antagonists, 35 cyclooxygenase-2 inhibitors associated with different diseases, [36][37][38][39][40][41][42][43][44] inhibitors of caspase-3 and caspase-7, 45 and voltage gated sodium channel modulators. 46 The synthesis of functionalized sulfonamides including substituted sultams has been reviewed by Majumdar and Mondal in 2011 47 and Ashfaq et al in 2013.…”

Targeting microsomal prostaglandin E2synthase-1 (mPGES-1): the development of inhibitors as an alternative to non-steroidal anti-inflammatory drugs (NSAIDs)

“…Two methods for measuring PGE 2 in the reaction mixture were established including the use of a PGE 2 ELISA kit 147 and LC-MS/MS. 148 Most importantly, this was a method for measuring PGE synthase with PGH 2 as a substrate, but PGH 2 is very labile and can be decomposed non-enzymatically into a mixture with PGE 2 and PGD 2 . Thus, it is important to separate the remaining unreacted PGH 2 from the newly formed PGE 2 in order to guarantee reliable results.…”