Isoxazolopyrimidinethione and Isoxazolopyridopyrimidinethione Derivatives: Key Intermediates for Synthesis of Novel Fused Triazoles as Potent 5-Reductase Inhibitors and Anti-Prostate Cancer

摘要

The arylideneisoxazolone derivative 1 is used for preparation of two different pyrimidinethiones 3 and 5 through interaction with thiourea and thiouracil, respectively. Compounds 3 and 5 were subjected to reaction with different hydrazonyl halides in basic medium to afford different triazolopyrimidines 9a, 9b, 9c, 9d, 9e, 9f, 9g, 9h and 13a, 13b, 13c, 13d, 13e, 13f, the structures were confirmed by their spectral and elemental analysis. All the newly synthesized products were screened against 5-reductase. Some of the newly synthesized compounds showed potent 5-reductase inhibition activities with good ED50.