Design, synthesis and biological activity assessment of phenoxybutyric acid derivatives as nonsteroidal 5α-reductase inhibitors / 南方医科大学学报
Journal of Southern Medical University
;
(12): 1830-1833, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-329190
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>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Butyrates
/
Drug Design
/
Chemistry
/
5-alpha Reductase Inhibitors
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2014
Type:
Article
Similar
MEDLINE
...
LILACS
LIS