Design, synthesis and biological activity assessment of phenoxybutyric acid derivatives as nonsteroidal 5α-reductase inhibitors

VernacularTitle:苯氧丁酸类非甾体5α-还原酶抑制剂的设计、合成及活性研究
Author: Kaixuan CHEN ¹ ; Zhenzhou JIANG ; Wenhua CHEN ; Baomin XI
Author Information

1. 南方医科大学药学院
Keywords: benign prostatic hyperplasia; 5α-reductase inhibitors; butyric acid
From: Journal of Southern Medical University 2014;(12):1830-1833
CountryChina
Language:Chinese
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. Results and Conclusion 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.