Synthesis and biological activity of N-acyl-5-bromanthranilic acids

Ten N-acyl-5-bromanthranilic acids have been obtained via acylation of 5-bromanthranilic acid with appropriate anhydrides. The antiinflammatory and antibacterial properties of the synthesized compounds have been evaluated. It is established that N-(o-anisoyl)-5-bromanthranilic acid possesses most pronounced antiinflammatory activity (49% inhibition of carrageenan induced paw edema in rat) and antimicrobial properties (MIC = 2.0 μg/ml with respect to St. aureus and E. coli). __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 40, No. 8, pp. 12–14, August, 2006.     

Dihydroretinoic acids and their derivatives. Synthesis and biological activity.

The syntheses of the ring and four side-chain dihydroretinoic acids and/or their esters, 3-7, are described. The syntheses of several other retinoids containing a substituted aromatic ring are also included. The biological activity of the compounds was evaluated in vivo in a chemically induced mouse skin papilloma test and in vitro in two vitamin A deficient assays. The activity observed for 1a, 1c, and 2a in the former test was partially retained in the dihydro derivatives 4b, 4c, and 6b. Similar results were found in the in vitro assays.     

Synthesis and biological activity of heterylamides of aroylpyruvic acids and 5-arylpyrazole-3-carboxylic acids

Communication XLVIII of the series: Chemistry of oxalyl derivatives of methyl ketones: for Communication XLVII, see [8].     

Synthesis and local anesthetic activity of substituted anilides of 6-methylpipecolinic acid

Translated from Khimiko-farmatsevticheskii Zhurnal, Vol. 23, No. 7, pp. 820–824, July, 1989.