Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors  

作　　者：Yuan Feng Tong Pei Zhang Feng Chen Ling Hua Hao Fei Ye Jin Ying Tian Song Wu 

机构地区：[1]Department of New Drug Research and Development (Key Laboratory of Biosynthesis of Natural Products, Ministry of Health of PRC), Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China [2]Department of Pharmacology, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China

出　　处：《Chinese Chemical Letters》2010年第12期1415-1418,共4页中国化学快报（英文版）

基　　金：Financial support was provided by the National Natural Science Funds for Young Scholar(No.30901841);the Research Fund for the Doctoral Program of Higher Education of China(No.200800231145);the Major Scientific and Technological Special Project for"Significant New Drugs Innovation"(No.2009ZX09301-003).

摘　　要：Based on the fact that petroselinic acid showed good inhibitory activity（IC50 = 6.99μmol/L） against protein tyrosine phophatase 1B（PTP1B） in vitro,a series of novel N-（alkoxyphenyl）-aminocarbonylbenzoic acid derivatives were designed and synthesized.The results indicated that most of the derivatives showed more potent activities against PTP1B.Especially,compound 13 had obvious activity with an IC50 of 106 nmol/L in vitro.Based on the fact that petroselinic acid showed good inhibitory activity（IC50 = 6.99μmol/L） against protein tyrosine phophatase 1B（PTP1B） in vitro,a series of novel N-（alkoxyphenyl）-aminocarbonylbenzoic acid derivatives were designed and synthesized.The results indicated that most of the derivatives showed more potent activities against PTP1B.Especially,compound 13 had obvious activity with an IC50 of 106 nmol/L in vitro.

关 键 词：Petroselinic acid PTP1B N-（Alkoxyphenyl）-aminocarbonylbenzoic acid derivatives SYNTHESIS Diabetes 

分 类 号：X835[环境科学与工程—环境工程] O636.1[理学—高分子化学]