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

Farmaco Sci. 1980 Sep;35(9):735-51.
[Article in Italian]

Abstract

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.

Publication types

  • English Abstract

MeSH terms

  • Amphetamine / antagonists & inhibitors
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anticonvulsants
  • Barbiturates / pharmacology
  • Behavior, Animal / drug effects
  • Body Temperature / drug effects
  • Chemical Phenomena
  • Chemistry
  • Drug Interactions
  • Guinea Pigs
  • In Vitro Techniques
  • Mice
  • Muscle Contraction / drug effects
  • Phenothiazines / chemical synthesis*
  • Phenothiazines / pharmacology
  • Quinolines / chemical synthesis*
  • Quinolines / pharmacology
  • Rats
  • Reserpine / antagonists & inhibitors

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Anticonvulsants
  • Barbiturates
  • Phenothiazines
  • Quinolines
  • Reserpine
  • Amphetamine