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Biological evaluation and synthesis of new pyrimidine-2(1H)-ol/-thiol derivatives derived from chalcones using the solid phase microwave method

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Twenty-five new hydroxy- and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20–34) and 4,6-diarylpyrimidine-2(1H)-thiol derivatives (35–44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1- one compounds (1–19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20–44) were evaluated with regard to their α-glucosidase activity. However, only compounds 22–25, 27, 31, 34, 35, 37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC50 values of the active compounds ranged between 2.36 and 13.34 µM. The 25 new compounds were also screened for their in vitro pancreatic lipase activity and compounds 20–27 and 35–39 were found to be active. |

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