A. Buttinoni, M. Ferrari, M. Colombo
Sep 1, 1983
Citations
0
Influential Citations
40
Citations
Quality indicators
Journal
Journal of Pharmacy and Pharmacology
Abstract
Indoprofen, (cw[4-(2-isoindoliny1-l-one)-phenyl] propionic acid) a non-steroidal analgesic anti-inflammatory drug (NSAID) (Buttinoni et a1 1973; Bruni et a1 1980) has an asymmetric carbon atom and can therefore occur either as the (+)or (-)-isomer. The optically active indoprofen enantiomers have been resolved (Tosolini et al 1974) and their absolute configurations determined (De Munari et a1 1980). Several workers have claimed that biological activity in some substituted phenylpropionic acids is due almost entirely to the (+)-isomer (Shen 1967; Ham et a1 1972; Takeguchi & Sih 1972; Tomlinson et a1 1972; Greig & Griffin 1975) believed to have the S-configuration (Wechter et a1 1974; Simmonds et a1 1980; Tamura et a1 1981). The aim of this study was to determine the contribution of the enantiomers to the activity and toxicity of racemic indoprofen. We also investigated their effect on prostaglandin biosynthesis, as the biological activity of this class of compounds is closely linked to inhibition of the prostaglandin system.