Synthesis and bioactivity of new Finasteride conjugate

	Synthesis and bioactivity of new Finasteride conjugate
	Zhao S ; Wu JZ ; Yang LJ ; Li Z ; Yu DH ; Li JF ; Yu J ; Liang YT ; Wang ES ; Fang XX
刊名	bioorganic & medicinal chemistry letters
	2011
卷号	21 期号:11 页码:3439-3442
关键词	BENIGN PROSTATIC HYPERPLASIA STEROID 5-ALPHA-REDUCTASE INHIBITORS MEN
ISSN号	0960-894x
通讯作者	wang es
中文摘要	finasteride is a synthetic 4-azasteroid compound that acts by inhibiting type ii 5 alpha-reductase, the enzyme that converts the androgen testosterone to 5 alpha-dihydrotestosterone. it was approved by the us fda for the treatment of benign prostatic hyperplasia and male pattern baldness. here the acylation product of finasteride c-18 amide n-polimod was synthesized by employing acylation reaction with polimod amide as a pivotal intermediate. the structure of the key intermediate and target molecule was confirmed by infrared spectrum, (1)h nmr and (13)c nmr spectra and mass spectrum, and the inhibition of the steroid 5 alpha-reductase and the rats' benign prostatic hyperplasia by the new finasteride conjugate and finasteride was also determined. the inhibition of the finasteride conjugate on 5 alpha-reductase was stronger than that of finasteride. prostate hyperplasia of rats was reduced by finasteride conjugate treatment similar to the finasteride treatment. however, the finasteride conjugate treated animals showed better viable condition than the finasteride treated ones, suggesting the new compound may have improved toxicity profile than finasteride. (c) 2011 elsevier ltd. all rights reserved.
收录类别	SCI收录期刊论文
语种	英语
WOS记录号	WOS:000290708300053
公开日期	2012-06-11
内容类型	期刊论文
源URL	[http://ir.ciac.jl.cn/handle/322003/44611]
专题	长春应用化学研究所_长春应用化学研究所知识产出_期刊论文
推荐引用方式 GB/T 7714	Zhao S,Wu JZ,Yang LJ,et al. Synthesis and bioactivity of new Finasteride conjugate[J]. bioorganic & medicinal chemistry letters,2011,21(11):3439-3442.
APA	Zhao S.,Wu JZ.,Yang LJ.,Li Z.,Yu DH.,...&Fang XX.(2011).Synthesis and bioactivity of new Finasteride conjugate.bioorganic & medicinal chemistry letters,21(11),3439-3442.
MLA	Zhao S,et al."Synthesis and bioactivity of new Finasteride conjugate".bioorganic & medicinal chemistry letters 21.11(2011):3439-3442.