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Background  Chalcones are intent in the daily diet as a favorable chemotherapeutic compound; on the other hand thiophene moiety is present in a large number of bioactive molecules having diverse biological efficiency.    Results  Our current goal is the synthesis of ( E )-1-(pyridin-3-yl)-3-(thiophen-2-yl) prop-2-en-1-one  3  that ’ s used as a starting compound to synthesize the novel pyrimidine-2-thiol, pyrazole, pyran derivatives. Chalcones  3  was prepared by condensation of 3-acetylpyridine with thiophene 2-carboxaldehyde which reacted with thiourea to obtain pyrimidinthiol derivative  4 . Compound  4  was allowed to react with hydrazine hydrate to afford 2-hydrazinylpyrimidine derivative  5 . Compound  5  was used as a key intermediate for a facile synthesis of the targets  6  and  7 . In contrast, pyranone  8  was obtained by transformation of compound  5 . Using as a precursor for the synthesis of new pyrazolo pyrimidine derivatives  9 – 10 . The major incentive behind the preparation of these compounds was the immense biological activities associated to these heterocyclic derivatives.    Conclusions  The newly synthesized compounds ( 1 – 4 ) showed potent anti-inflammatory activities both in vitro and in vivo. They also exhibited promising antioxidant vitalities against α, α-diphenyl-β-picrylhydrazyl scavenging activity and lipid peroxidation. In conclusion, compound  1  showed a hopefully anti-inflammatory and antioxidant activities.

Heterocyclization of polarized system: synthesis, antioxidant and anti-inflammatory 4-(pyridin-3-yl)-6-(thiophen-2-yl) pyrimidine-2-thiol derivatives