发明名称 |
DERIVATIVES OF NAFTIFINE HYDROCHLORIDE, AND PREPARATION METHOD AND USE THEREOF |
摘要 |
Disclosed in the present invention are derivatives of naftifine hydrochloride, and a preparation method and use thereof. The derivatives of naftifine hydrochloride of the present invention have a structure as shown by formula (I), wherein Ar has the definition as described in the description and claims. By inhibiting the expression and/or function of key catalyzing enzyme CrtN in a golden yellow pigment synthesis pathway and powerfully inhibiting the synthesis of golden yellow pigments, the virulence of bacteria can thus be lowered. The key catalyzing enzyme CrtN in the golden yellow pigment synthesis pathway can be used as a drug target; and compounds capable of inhibiting the expression and/or function of the catalyzing enzyme CrtN can be used for preparing anti-bacterial drugs. The naftifine hydrochloride and the derivatives thereof in the present invention can be used as inhibitors for the catalyzing enzyme CrtN to powerfully inhibit the synthesis of golden yellow pigments, so that the virulence of Staphylococcus aureus can be lowered, and same can thus be used for preparing the anti-bacterial drug, and especially a drug for resisting Staphylococcus aureus infections. |
申请公布号 |
WO2015168979(A1) |
申请公布日期 |
2015.11.12 |
申请号 |
WO2014CN81369 |
申请日期 |
2014.07.01 |
申请人 |
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES;EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY |
发明人 |
LAN, LEFU;LI, JIAN;CHEN, FEIFEI;WANG, YOUXIN;JIANG, HUALIANG |
分类号 |
A61K31/137;A61P31/04;C07C209/00;C07C209/08;C07C211/30;C12N1/20;C12Q1/14;C12R1/445 |
主分类号 |
A61K31/137 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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