Synthesis, Characterization, and Biological Activity of Some Aza-Uracil Derivatives

Thiation of 1 by LR gave the corresponding 3,5-dithioxo derivative 2 and the trimer 3. Methylation of 1 afforded the S-methyl derivative 4. Compound 1 was fused with 6-bromo-2-phenyl-benzo[1,3-d] oxazin-4-one (5) and gave 6. Condensation of 1 with some acid derivatives 7a-d and/or 8a-c yielded thiadiazolo-triazine derivatives 9a-d and 10a-c. Compounds 9a,c and 10c were hydrolyzed to furnish 11a-c. Acetylation of 14 afforded mono-and diacetyl-derivatives 15 and 16. Benzoylation of 14 afforded mono-and dibezoyl-derivatives 17 and 18. 14 with some aromatic aldehydes yielded 19a-c. Reacting 14 with phenyl (iso-and/or isothio-) cyanate gave the urea derivatives 20a,b. Thiation of 14 with P(4)S(10) furnished 21. The newly synthesized compounds were tested as antimicrobial agents.