Anti-inflammatories

Among the indole derivatives which have found use as drugs are indo-methacin, one of the first non-steroidal anti-inflammatory agentsfll], sumatriptan, which is used in the treatment of migraine headaches[12] and pindolol[13], one of the p-adrenergic blockers. 

One of the virtues of the Fischer indole synthesis is that it can frequently be used to prepare indoles having functionalized substituents. This versatility extends beyond the range of very stable substituents such as alkoxy and halogens and includes esters, amides and hydroxy substituents. Table 7.3 gives some examples. These include cases of introduction of 3-acetic acid, 3-acetamide, 3-(2-aminoethyl)- and 3-(2-hydroxyethyl)- side-chains, all of which are of special importance in the preparation of biologically active indole derivatives. Entry 11 is an efficient synthesis of the non-steroidal anti-inflammatory drug indomethacin. A noteworthy feature of the reaction is the... 

Hydroxybenzaldehydes readily react with compounds containing methyl or methylene groups bonded to one or two carboxyl, carbonyl, nitro, or similar strong electron-withdrawing groups. The products are usually P-substituted styrenes. 4-Hydroxybenzaldehyde, for example, reacts with 2-methylquinazolines (where R = H, Cl) to give compounds which have anti-inflammatory activity (59). 

Alkan olamines are used in the manufacture of a variety of pharmaceutical compounds. Some of these products include antitumor agents, anti-inflammatory and allergy agents, and anticonvulsants. The Hterature reports ethan olamine derivatives in the treatment of Alzheimer s disease (216), the treatment of cerebral psychoorganic syndromes (217), and veterinary dmgs (218). 

The anti-inflammatory agent Oxapro2in, 2-(4,5-diphenyl-2-oxa2ole)propionic acid mono aluminum and dihydroxyalurninum salts, is made by reaction of the sodium salt with aluminum sulfate under controlled conditions (96). Again, the aluminum salts of many carboxylic acid based dmgs are less irritating, ulcerous, and/or toxic, and have a more pleasant taste than their parent acids. 

In addition, various pyridopyridazines have been claimed to have activity as antibacterials and antiseptics, antitubercular agents, analgesics, anti-inflammatories, antiallergics, tranquillizers, CNS depressants and muscle relaxants. 

High anti-inflammatory activity has been found for 3,3-dialkyl-l-aminoazetidine-2,4-dione derivatives such as (204) (64HC(19-2)885). 

Alkanes, dipurin-8-yl-synthesis, 5, 574 Alkanes, poly-N-pyrazoIyl-synthesis, 5, 320 Alkanoic acids, tetrazolyl-anti-inflammatory activity, 5, 835 Alkanoic acids, 4-thienyi-cyclization, 4, 905-906 Alkene metathesis mechanism, 1, 668 Alkenes activated... 

Tetrazole, 5-phenoxy-l -phenyl-mass spectra, 5, 801 photolysis, 5, 811 Tetrazole, 1-phenyl-deuterium-hydrogen exchange, 5, 806 mercuration, 5, 59 NMR, 5, 798 tautomerism, 5, 804 UV spectra, 5, 798 Tetrazole, 2-phenyl-NMR, 5, 798 tautomerism, 5, 804 UV spectra, 5, 798 Tetrazole, 5-phenyl-alkylation, 5, 818 anti-inflammatory activity, 5, 835 blowing agent, 1, 410 reactions... 

Benzoyl-2,3-dihydro-lH-pyrrolizine-l-cai boxylic acid (ketorolac, L ) and 2-(3-benzoyl-phenyl)propionic acid (ketoprofen, L ) ai e biologically activ ligands used in medicine as non-steroidal anti-inflammatory dmgs. 

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