Individuals exposed to carcinogenic aromatic amines excrete arylamine Nand O-glucuronide metabolites. This study assessed the susceptibility of selected glucuronides to hydrolysis by human and Escherichia coli b-glucuronidase. Nor O-glucuronides were prepared with the following aglycones: benzidine, N-acetylbenzidine, N*-hydroxy-N-acetylbenzidine, N-hydroxy-N-acetylbenzidine, N-hydroxy-N,N*-dia...

N-Hydroxy-T-fluoro^-acetylaminofluorene (A^-hydroxy-7fluoro-AAF) and Ar-hydroxy-2-acetylaminophenanthrene (A7hydroxy-AAP) were identified as urinary metabolites of 7-fluoro2-acetylaminofluorene and 2-acetylaminophenanthrene, respectively, in the rat. When administered as 0.010-0.012% of the diet for 10-15 weeks AT-hydroxy-7-fluoro-AAF proved to be a much more potent carcinogen for the rat than ...

A series of eight substituted bis-2-hydroxy-1,4-naphthoquinone derivatives was synthesized through lawsone condensation with various aromatic and aliphatic aldehydes under mild acidic conditions. The title compounds were evaluated for antileishmanial activity in vitro against Leishmania amazonensis and Leishmania braziliensis promastigotes; six compounds showed good activity without significant...

Co-metabolism of 3-methylcatechol, 4-chlorocatechol and 3,5-dichlorocatechol by an Achromobacter sp. was shown to result in the accumulation of 2-hydroxy-3-methylmuconic semialdehyde, 4-chloro-2-hydroxymuconic semialdehyde and 3,5-dichloro-2-hydroxymuconic semialdehyde respectively. Formation of these products indicated that cleavage of the aromatic nucleus of the substituted catechols was acco...

A mild and efficient method for the synthesis of optically active α-hydroxy acids through chemoselective oxidation of monosubstituted ethylene glycols using the TEMPO-NaOCl reagent system is described. It is evident from our studies that the solvent, pH and reaction temperature are very crucial for the success of this oxidation. The versatility of this method has been demonstrated with a variet...

Twenty Baylis-Hillman adducts were synthesized from different aromatic aldehydes and activated vinyl derivatives. The adducts, which are differently substituted 3-hydroxy-2-methylene-3-phenylpropionic acid derivatives, were screened for their antimicrobial activity in vitro by the serial dilution method. Many of these molecules displayed potent antibacterial and antifungal activities. The ease ...

Individuals exposed to carcinogenic aromatic amines excrete arylamine N- and O-glucuronide metabolites. This study assessed the susceptibility of selected glucuronides to hydrolysis by human and Escherichia coli beta-glucuronidase. N- or O-glucuronides were prepared with the following aglycones: benzidine, N-acetylbenzidine, N'-hydroxy-N-acetylbenzidine, N-hydroxy-N-acetylbenzidine, N-hydroxy-N...