Synthesis and characterization of some new uracil derivatives and their biological activity

Abstract EN

This research includes the synthesis of thirty derivatives of uracil.

Nucleophilic substitution reaction (thiol, alkylation, hydrazine, thioacid,..

etc) of 4-chlorouracil afforded the corresponding derivatives.

The 4-(2`-thiol-1`, 3`, 4`-oxadiazole-5`-thiomethyl) uracil (12),) N` - phenyl – 2` - thio -1`, 3`, 4`-triazole-5`-methyl)-(2, 6-dihydroxy-4-pyrimidinyl) sulphide (14) and 5-(2`, 6`-dihydroxy-4`-pyrimidinyl thioacetamido)-1, 3, 4-thiadiazole-2-thiol (15), were synthesized by treatment of 4-thioacetichydrazide uracil (11) with carbon disulfide in the presence of a base or phenylisothiocyanate in the presence of base.

Mannich bases of alkynyl thio derivativeis (3a and 10) were synthesized by the reaction of paraformaldehyde and secondary amine in the presence of CuCl (19a,b and 20a,b).

These compounds were characterized by spectroscopic methods (IR and UV), by their elemental analysis (C, H, N) and Rf values.

Biological activity of the synthesized compounds was determined.