Peptidomimetics as Potent and Selective PTP1B Inhibitors#

被引：1

作者：

Patel, Dipam ^{[1
,2
]}

Jain, Mukul ^{[1
]}

Shah, Shailesh R. ^{[2
]}

Bahekar, Rajesh ^{[1
]}

Jadav, Pradip ^{[1
]}

Shah, Kiran ^{[1
]}

Joharapurkar, Amit ^{[1
]}

Shaikh, Mubeen ^{[1
]}

Sairam, Kalapatapu V. V. M. ^{[1
]}

机构：

[1] Zydus Res Ctr, Ahmadabad 382210, Gujarat, India

[2] Maharaja Sayajirao Univ Baroda, Fac Sci, Dept Chem, Vadodara 390002, India

来源：

MEDICINAL CHEMISTRY | 2013年 / 9卷 / 05期

关键词：

Tri-peptides; pTyr mimetics; PTP1B inhibitors; TCPTP; Type; 2; diabetes; Metabolic disorders; TYROSINE-PHOSPHATASE; 1B; MOLECULAR-BASIS; DISCOVERY; INSULIN; RESISTANCE; OBESITY; SITE;

D O I：

10.2174/1573406411309050005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.

引用

页码：660 / 671

页数：12

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