Asimple laboratory method for preparing 8-amino-substituted 7-(2-aryl-2-oxoethyl)xanthines by reacting the corresponding 8-bromo derivatives with primary and secondary amines in ethoxyethanol was developed. The structures of the synthesized compounds were confirmed by PMR spectroscopy. The analgesic and anti-inflammatory activities of the synthesized compounds were studied in laboratory animal tests. It was established that the majority of the tested compounds possessed moderate or strong analgesic and anti-inflammatory activities. Several compounds exhibited activity stronger than or comparable to that of metamizole sodium (analgin) and diclofenac. 7-(2-Oxo-2-phenylethyl)-8-(4-methylpiperidinyl-1)theophylline (XIV) and 7-(2-oxo-2-phenylethyl)-8-(4-ethylpiperazinyl-1)-3-methylxanthine (XVII) could be introduced as analgesic and anti-inflammatory agents after detailed pharmacological testing.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 48, No. 8, pp. 24 – 27, August, 2014.
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Romanenko, N.I., Nazarenko, M.V., Kornienko, V.I. et al. Synthesis and Physicochemical and Biological Properties of 8-Amino-Substituted 7-(2-Aryl-2-Oxoethyl)Xanthines. Pharm Chem J 48, 509–512 (2014). https://doi.org/10.1007/s11094-014-1142-3
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DOI: https://doi.org/10.1007/s11094-014-1142-3