New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative.

This work describes the utility of pyrazole-4-carbaldehyde as starting material for the synthesis of a novel potent series of 5α-reductase and aromatase inhibitors derived from 1,2,3-triazole derivative. Condensation of with active methylene and different amino pyrazoles produced the respective Schiff bases -, and . On the other hand, was reacted with ethyl cyanoacetate and thiourea in one-pot reaction to afford the pyrazolo-6- thioxopyridin-2-[3]-one (). Moreover, α-β unsaturated chalcone derivative was prepared via the reaction of compound with -methoxy acetophenone, which in turn reacted with each of ethyl cyanoacetate, malononitrile, hydrazine hydrate, and thiosemicarbazide to afford the corresponding pyridine and pyrazole derivatives , , and The structure of newly synthesized compounds was characterized by analytical and spectroscopic data (IR, MS and NMR) All new compounds were evaluated against 5α-reductase and aromatase inhibitors and the results showed that many of these compounds inhibit 5α-reductase and aromatase activity; compound was found to be the highest potency among the tested samples comparing with the reference drugs.