As a part of our continuous research in the area of click approach, we have designed and synthesized several new S-methyleme bridge 1,2,3-triazolyl pyrimidinone through incorporating triazole moiety with the pyrimidine ring. Novel triazoles, based on thieno[2,3-d]-pyrimidines, were synthesized from 2-aminothiophen esters using a one-pot process, and convergent construction of complex molecules without the isolation of intermediates under well-known click approach conditions. The structure of the synthesized compounds confirmed by spectral and analytical data. The synthesized 1,2,4-triazolo compounds were screened for their PDE 5 inhibitory activity and showed encouraging activity compared to sildenafil as a reference drug. These compounds open new opportunities for the rational design of new PDE 5 inhibitors with comparable activity to sildenafil.

Synthesis of fused and isolated triazoles based on thieno[2,3-d]pyrimidines and the screening of their PDE 5 inhibitory activity

255th National Meeting (2018)

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