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Discovery of Highly Polar beta-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors

文献类型：期刊论文

作者Huang, Fubao1,3; Ning, Mengmeng1,3; Wang, Kai1,3; Liu, Jia3; Guan, Wenbo1,2,3; Leng, Ying1,2,3; Shen, Jianhua1,3
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2019-12-12
卷号62期号:23页码:10919-10925
ISSN号0022-2623
DOI10.1021/acs.jmedchem.9b01649
通讯作者Leng, Ying(yleng@simm.ac.cn) ; Shen, Jianhua(jhshen@simm.ac.cn)
英文摘要Although intensively expressed within intestine, the precise roles of intestinal dipeptidyl peptidase IV (DPPIV) in numerous pathologies remain incompletely understood. Here, we first reported a nonsystemic intestine-targeted (NSIT) DPPIV inhibitor with beta-homophenylalanine scaffold, compound 7, which selectively inhibited the intestinal rather than plasmatic DPPIV at an oral dosage as high as 30 mg/kg. We expect that compound 7 could serve as a qualified tissue selective tool to determine undetected physiological or pathological roles of intestinal DPPIV.
WOS关键词GUT MICROBIOTA ; MEDICINAL CHEMISTRY ; COLITIS ; MECHANISMS ; POTENT ; HEART
资助项目State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica[SIMM1903ZZ-02]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000503114200025
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/282261]  
专题新药研究国家重点实验室
通讯作者Leng, Ying; Shen, Jianhua
作者单位1.Chinese Acad Sci, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Huang, Fubao,Ning, Mengmeng,Wang, Kai,et al. Discovery of Highly Polar beta-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2019,62(23):10919-10925.
APA Huang, Fubao.,Ning, Mengmeng.,Wang, Kai.,Liu, Jia.,Guan, Wenbo.,...&Shen, Jianhua.(2019).Discovery of Highly Polar beta-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,62(23),10919-10925.
MLA Huang, Fubao,et al."Discovery of Highly Polar beta-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 62.23(2019):10919-10925.

入库方式： OAI收割

来源：上海药物研究所

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