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Introduction. New potential biologically active compounds with different pharmacological activities were found among pyrimidine derivatives. Simple and available synthesis of tetrahydropyrimidine-5-carboxamides was developed in Perm State Pharmaceutical Academy. Products of this reaction previously shown high analgesic and anti-inflammatory activities.Aim. To get previously unknown functionalized pyrimidines and to study their analgesic, anti-inflammatory and antipyretic activities.Materials and methods. 11 compounds N,6-diaryl-4-methyl-2-thioxo-1,2,3,6-tetrahydropyrimidine-5-carboxamides are objects of research. Their structure has been confirmed by spectroscopy methods. The biological activities were carried out by recommended methods for preclinical study of new pharmacological substances.Results and discussion. This paper presents the results of preclinical tests of the obtained compounds.Conclusion. Some compounds demonstrated high analgesic, anti-inflammatory and antipyretic activities and could be recommend for further study as perspective non-steroidal drugs.

Изучены особенности строения и исследована противовоспалительная активность 13-(N-ариламинокарбонил)-9-метил-11-тиоксо-8-окса-10,12-диазатрицикло[7.3.1.02,7]тридека-2,4,6-триенов и их 10-N-фенилпроизводных. Обнаружено, что данные соединения обладают высокой противовоспалительной активностью и могут быть отнесены к классу перспективных нестероидных противовоспалительных средств.

The Biginelli reaction [1][2][3] has been recognized as a key method to prepare the substituted 3,4-dihydropyrimidine-2(1H)-ones(thiones); such compounds have exhibited antiviral [4], antitumor [5], anti-inflamematory [6], anti-tubercular [7], and antimicrobial [8] activity. In view of this, further development of this reaction as a facile, convenient, and safe procedure to prepare new low-toxic potentially biologically active pyrimidine derivatives is of special interest [9-12].The Biginelli reaction involving cyanoguanidine has been only once described [5]; the reaction has been performed in the presence of catalytic amount of paratoluenesulfonic acid to yield 35% of 2-imino-4methyl-3-cyano-6-phenyl-N-2-chlorophenyl-1,2,3,6tetrahydropyrimidine-5-carboxamide.Keeping in mind the high pharmaceutical importance of pyrimidine derivatives and potential antitumor activity of cyano-containing compounds [13], in this work we studied the interaction of acetoacetic acid N-arylamides with cyanoguanidine and aromatic aldehydes in order to elaborate the preparative procedure of cyanopyrimidines synthesis avoiding any toxic compounds.It was found that the reaction occurred in bulk in the absence of any catalyst to afford N,6-diaryl-2imino-4-methyl-3-cyano-1,2,3,6-tetrahydropyrimidine-5-carboxamides I-X with yields of 69-78% (Scheme 1).The compounds I-X were colorless of lightly colored substances soluble in DMSO, DMF, acetic acid, and ethanol but insoluble in water. The products structures were confirmed by means of 1 Н NMR, 13 С NMR, and IR spectroscopy as well as mass spectrometry. Splitting of the signals of pyrimidine protons in positions 1 and 6 evidenced the reaction

Реакция N,6-диарил-4-метил-2-тиоксо-1,2,3,6-тетрагидропиримидин-5-карбоксамидов с этиловым эфиром хлоруксусной кислоты приводит к гидрохлоридам N,5-диарил-7-метил-3-оксо-2,3-дигидро-5H-[1,3]тиазоло[3,2-a]пиримидин-6-карбоксамидов. Среди синтезированных соединений найдены вещества, проявляющие противомикробную активность.