Design, synthesis and biological activity assessment of phenoxybutyric acid derivatives as nonsteroidal 5α-reductase inhibitors / 南方医科大学学报

ABSTRACT

<p><b>OBJEVTIVE</b>To synthesize phenoxybutyric acid derivatives as 5α-reductase inhibitors and test their biological activities in vitro.</p><p><b>METHODS</b>Eight analogues as nonsteroidal 5α-reductase inhibitors were designed and synthesized by substitution reaction of 6-(4-phenyl-piperazine-1-yl)-3(2H)-pyridazinone with phenoxybutyric acid derivatives.</p><p><b>RESULTS AND CONCLUSION</b>The structures of the compounds were characterized by 1H-NMR and MS. Biological evaluation indicated that 7 out of the 8 compounds exhibited moderate 5α-reductase inhibitory activities, especially the compounds A1 and A7 with inhibition rates reaching 12.50% and 19.64% at the concentration of 3.3 × 10⁻⁵ mol/L, respectively.</p>