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Pyrimidine derivativesPyrimidine derivatives R 0510 (6-Methyl-2-methylsulfanyl-4-oxo-3,4-dihydro-3-pyrimidinyl)acetic Acid and Related Compounds Exhibiting Antiinflammatory Activity. -The title acid (IV) and its amination products (VI) and (VIII) are synthesized and evaluated for their antiinflammatory activities. Most of the compounds obtained are found to be more active than acetylsalicylic acid and some of them, e.g. (IV), (VI) and (VIIIa) are significantly more active than ibuprofen. -(JAKUBKIENE*, V.; BURBULIENE, M. M.; UDRENAITE, E.; GARALIENE, V.; VAINILAVICIUS, P.; Pharmazie 57 (2002) 9, 610-613; Chem. Fac., Univ. Vilnius, Vilnius 2006, Lithuania; Eng.) -D. Singer 01-150

Several derivatives of the title compound (I) are prepared, e.g. S-alkylated derivatives (V), N-substituted derivatives (III) and (VIII), triazoles (IX) and (XIII), thiocarbohydrazides (X) and (XII). Most of the derivatives obtained are less toxic and show higher antiinflammatory activity than the reference drugs acetylsalicylic acid and ibuprofen. The most active derivatives are compounds (Vb) and (VIIIb). -(MEKUSKIENE, G.; BURBULIENE, M. M.; JAKUBKIENE, V.; UDRENAITE, E.; GAIDELIS, P.; VAINILAVICIUS, P.; Chem. Heterocycl.

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Treatment of 5-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-3-pyrimidinyl)-methyl-1,3,4oxadiazole-2-thione with haloalkanes yielded oxadiazole S-alkyl derivatives, whereas its reaction with formaldehyde and amines resulted in formation of oxadiazole N(3)-aminomethyl derivatives. The alkylation of 2-alkylsulfanyl-5-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-3-pyrimidinyl)-methyl-1,3,4-oxadiazoles with methyl bromoacetate proceeded at the N(1)-position of pyrimidine to give 2-alkylsulfanyl-5-(1-methoxycarbonylmethyl-6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-3-pyrimidinyl)-methyl-1,3,4-oxadiazoles, whereas aminomethylation, bromination, or nitration took place at position 5 of pyrimidine ring and afforded the corresponding 5-pyrimidine substituted derivatives.