Synthesis and anti-inflammatory activity of carboxy-phenylamides 1-oxides of nicotinic and isonicotinic acids / Danilenko V.F., Portnyagina V.A., Klebanov B.M., Ryabukha T.K. // Russian Pharmacology and Toxicology. - 1979. - V. 42, l. 4. - P. 164-168.

ISSN:
00360325
Type:
нет данных
Abstract:
The purpose of the present study was to synthesise and examine the physiological activity of new carboxyphenylamides of 1-oxides nicotinic and isonicotinic acids. The test compounds carboxyphenylamides of nicotinic and isonicotinic acids are of low toxicity: their LD50 was between 765 and 2000 mg/kg. The toxic action is a function of chemical structure: in nicotinic and isonicotinic acid derivatives, a shift of the carboxyl group from ortho, into the meta and para-position in the phenyl ring reduces the toxicity. All of the test compounds exhibited some degree of anti-exudative action. The most active in this respect were the para-substituted derivatives. All of the test compounds displayed analgesic properties, the degree of which was most pronounced in the 1-oxide of p-caroxyphenylamide derivative of isonicotinic acid. The test compounds also exhibited antipyretic properties, by lowering rectal temperature in rats during lactic fever; however, this effect showed no clear relationship with the actual chemical structure in this series of compounds.
Author keywords:
Index keywords:
antiinflammatory agent; antipyretic analgesic agent; nicotinic acid derivative; adverse drug reaction; animal experiment; drug administration; drug analysis; drug screening; drug synthesis; drug toxic
DOI:
нет данных
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Affiliations Kiev Pharmacol. Toxicol. Res. Inst. UkrSSR, Min. Hlth, Kiev, Russia
CODEN RPTOA
Language of Original Document English
Abbreviated Source Title RUSS. PHARMACOL. TOXICOL.
Source Scopus