Design, synthesis and biological activity assessment of phenoxybutyric acid derivatives as nonsteroidal 5α-reductase inhibitors.
- Author:
Kaixuan CHEN
1
;
Zhenzhou JIANG
;
Wenhua CHEN
;
Baomin XI
Author Information
- Publication Type:Journal Article
- MeSH: 5-alpha Reductase Inhibitors; chemical synthesis; pharmacology; Butyrates; chemistry; pharmacology; Drug Design
- From: Journal of Southern Medical University 2014;34(12):1830-1833
- CountryChina
- Language:Chinese
-
Abstract:
OBJEVTIVETo synthesize phenoxybutyric acid derivatives as 5α-reductase inhibitors and test their biological activities in vitro.
METHODSEight 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 CONCLUSIONThe 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.
