The Effect of 4-Substituent of Benzoic Acid on Glycine Conjugation

The relationship between the glycine conjugation of 4-substituted derivatives of benzoic acid and physico-chemical property was studied using rats. A linear relationship was found between the lipophilicity and the glycine conjugation after the intravenous injection of the derivative into rats. But t...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1990/06/25, Vol.38(6), pp.1753-1754
Hauptverfasser:	NANBO, Toshio, FUKASAKU, Noboru, YAMAGUCHI, Michio, TAKAGI, Hideyuki, UEDA, Takao, YOKOSHIMA, Tetsuyoshi
Format:	Artikel
Sprache:	eng
Schlagworte:	4-substitution benzoic acid Biological and medical sciences glycine conjugation Medical sciences Miscellaneous partition coefficient permeability superdelocalizability Toxicology
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Beschreibung
Zusammenfassung:	The relationship between the glycine conjugation of 4-substituted derivatives of benzoic acid and physico-chemical property was studied using rats. A linear relationship was found between the lipophilicity and the glycine conjugation after the intravenous injection of the derivative into rats. But there was no relationship between the lipophilicity and permeability into the liver. The formation of the glycine conjugate using mitochondria fraction of the liver was responsible for the superdelocalizability indicating the electrophilicity of carboxyl carbon.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.38.1753