Design and synthesis of new 1,8 disubstituted purine 2,6 diones and 3,6 disubstituted thiazolo[2,3 f]purine 2,4 diones as potential antinociceptive and antiinflammatory agents.

personАвтори: Alaa M. Hayallah


In this study, the design, synthesis and preliminary pharmacological investigation of novel 8-(2-oxo-2-p-(un)substituted phenyl)-1-substituted-3,7,8,9-tetrahydropurine-2,6-diones (11-20) and 3,6-disubstituted thiazolo[2,3-f]purine-2,4-diones (21-30) are described. 1,8-Disubstituted purine-2,6-dioneswerepreparedby thereactionof3-substituted-8-thioxo-3,7,8,9-tetrahydropurine-2,6-diones-(4-5) with appropriate phenacyl bromides (6-10). Compounds (4-5) were in turn prepared by reaction of 3-substituted-5,6-diaminouracils (3a-b) with carbon disulfide. The derivatives (21-30) were obtained by cyclodehydration of compounds (11-20) in polyphosphoric acid (PPA). The effect of the new prepared derivatives as potential antinociceptive and anti-inflammatory agents was carried out on mice and rats. Aspirin and indomethacin were used as reference drugs. Some of the tested compounds have shown a pronounced analgesic and antiinflammatory activity. The results here illustrate a promising analgesic and antiinflammatory activity of the newly synthesized derivatives.

Етикети: , , , , ,