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The biological activity of several lupane and oleanane β-enaminoketones was studied. Comparative analysis of leukocyte reactions showed that both groups of triterpene derivatives had high biological activity on chronic administration and that their immunosuppressive activity resulted from toxic effects on lymphocytes.
The immunotropic effect of the 2,3-seco derivatives of allobetulon, betulonic acid, and the methyl ester of betulonic acid were studied. It was found that the highest activity is shown by compounds with an oleanane fragment. The presence of a free C28-carboxyl group enhances the activity of lupane 2,3-seco derivatives. A significant contribution to the(More)
The biological activity of a series of new amino derivatives of dehydroabietic acid has been studied. 12-N,N-Diethylaminoacetyl-8,11,13-abietatrien-18-oate hydrochloride produces a calming effect, shows pronounced anxiolytic activity, and exhibits antipyretic action comparable with that of the reference drug (analgin).
Substituted amides and hydrazides of dialkylaminoacetic and arylaminoacetic acids are peptidomimetics and exhibit biological activity [1, 2]. Recently [3], we described the synthesis and some biological effects of N-[2-( p-hydroxyphenyl)-1,1-dialkylethyl]amides of some carboxylic acids. In continuation of investigations in this direction, we report on the(More)
As is known, the ulcerogenic properties of nonsteroidal antiinflammatory drugs is a factor limiting their use in clinics. It was established that the side effects can sometimes be reduced by attaching a pharmacophore fragment to a natural amino acid residue. In this context, we have synthesized ibuprofen amides (I – III) by the condensation of ibuprofen(More)
Nonsteroidal anti-inflammatory drugs and non-narcotic analgesics are widely used to treat various inflammatory diseases of infectious and noninfectious nature [1]. The development of new drugs based on terpenophenols, which have a unique set of pharmacological properties [2], is highly promising. The literature teaches that phenols with a bicyclic isobornyl(More)
As is known, the structural modification of well-known antiinflammatory compounds (ibuprofen, indomethacin, etc.) by reactions with amino acids sometimes leads to an increase in the main pharmacological effect, a decease in toxicity, and a change in the mechanism of antiinflammatory action of the derivatives [1 – 10]. The purpose of this study was to(More)
The reactions of substituted arenes with isobutyric aldehyde and methylthiocyanate yield 1-methylthio-3,4-dihydroisoquinolines. The subsequent treatment with AcOH/AcONa yields 2H-3,3-dimethyl-3,4-dihydroisoquinolin-1-ones, some of which exhibit pronounced antiinflammatory and analgesic properties.