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By by Helmut Buschmann (Editor), Thomas Christoph (Editor), Elmar Friderichs (Editor), Corinna Maul (Ed

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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.

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