By by Helmut Buschmann (Editor), Thomas Christoph (Editor), Elmar Friderichs (Editor), Corinna Maul (Ed
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Extra resources for Analgesics: From Chemistry and Pharmacology to Clinical Application
6). The compound showed inhibition of prostaglandin synthesis in inflammatory cells and was largely free of unwanted gastrointestinal effects in animal models. Moreover, NS-398 did not affect prostaglandin production in the stomach or kidney. On recognizing that NS-398 was a more or less preferential selective inhibitor of COX-2, new interest In this class of anti-inflammatory agents evolved. Nimesulide and flosulide are two other compounds with a diaryl ether and thioether structure, respectively, which bear a methansulfonanilide moiety.
Fatty acid and eicosanoids bind to PPAR and regulate transcription. PPAR activation inhibits monocyte differentiation and expression of several pro-inflammatory genes such as iNOS, TNF, etc. PPAR activation inhibits tumor cell proliferation (epithelial, colon, prostate). PPAR is involved in angiogenesis. \ Figure 19: Mechanism of action of NSAIDs as enzyme inhibitors and/or transcriptional regulators. ) Pd-C/H2/CH3COOH 0 COOH Scheme 4: Synthesis of acemetacin. The reaction product of indomethacin (see below) with benzyl bromo acetate can also be hydrogenated to Acemetacin.
Replacement of the methylsulfonyl group by a sulfonamide group reduces COX-2 selectivity but improves oral bioavailability. g. pyrrole, thiazole, °xaz°'e. furane, furanone, imidazole, isoxazole, pyrimidine, thiophene, pyrazole, cyclopentenone O — S-NH2 6 R ~S-CH3 • 6 Scheme 3: General structure of carbocycles and heterocycles with vicinal aryl substituents. The structural pre-requisites shown are obligatory for enhanced activity towards COX-2. 2 Cyclooxygenase Inhibition 27 Diaryl- or aryl-heteroaryl-ethers and thioethers HN" F HN^ Ck N02 N02 O' Nimesulid NS-398 0^,0 HNX "~ Flosulid V °st°NH HN H3C V s CH3 F /S.