title: [Design, synthesis and biological activity assessment of phenoxybutyric acid derivatives as nonsteroidal 5α-reductase inhibitors].
abstract: OBJECTIVE
  To synthesize phenoxybutyric acid derivatives as 5α-reductase inhibitors and test their biological activities in vitro.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: College of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, China.E-mail: Chenkx1988@163.com.
authors.forename: Kaixuan
authors.initials: K
authors.lastname: Chen
authors.forename: Zhenzhou
authors.initials: Z
authors.lastname: Jiang
authors.forename: Wenhua
authors.initials: W
authors.lastname: Chen
authors.forename: Baomin
authors.initials: B
authors.lastname: Xi
mesh_terms: D058891:5-alpha Reductase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D002087:Butyrates / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design
chemical_list: D058891:5-alpha Reductase Inhibitors; D002087:Butyrates