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  • [Derivatives of 2-phenothiazin-2'-yl-cinchoninic acid with analgesic and anti-inflammatory activity].

[Derivatives of 2-phenothiazin-2'-yl-cinchoninic acid with analgesic and anti-inflammatory activity].

Il Farmaco; edizione scientifica (1980-09-01)
F Sparatore, F Savelli, G Cordella
摘要

In order to investigate the effects of the overlapping of cinchophene and phenothiazine structures, connected with antiinflammatory and analgesic activities, several derivatives of 2-phenothiazin-2'-yl-cinchoninic acid were prepared through the condensation of isatin or 5-substituted isatins with 2-acetylphenothiazine or its 10-ter-aminoalkyl derivatives. Most of these compounds exhibit analgesic activity, but only a few, of those so far tested, show antiinflammatory activity. Compound (G) with R' = H, R" = C2H5 and R"' = dimethylaminoethyl shows analgesic activity corresponding to 88% of that of phenylbutazone. Moreover some compounds show signs of sympatholytic and vasodilatatory activities and also bactericidal and amebicidal properties in vitro, while some others demonstrate a modest neuroplegic activity.

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Sigma-Aldrich
2-乙酰基吩噻嗪, 95%