Discovery of Orally Active, Potent, and Selective Benzotriazole-Based PTP1B Inhibitors

被引：25

作者：

Patel, Dipam ^{[1
,2
]}

Jain, Mukul ^{[1
]}

Shah, Shailesh R. ^{[2
]}

Bahekar, Rajesh ^{[1
]}

Jadav, Pradip ^{[1
]}

Darji, Brijesh ^{[1
]}

Siriki, Yernaidu ^{[1
]}

Bandyopadhyay, Debdutta ^{[1
]}

Joharapurkar, Amit ^{[1
]}

Kshirsagar, Samadhan ^{[1
]}

Patel, Harilal ^{[1
]}

Shaikh, Mubeen ^{[1
]}

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

Patel, Pankaj ^{[1
]}

机构：

[1] Zydus Res Ctr, New Drug Discovery Div, Dept Med Chem, Ahmadabad 382210, Gujarat, India

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

来源：

CHEMMEDCHEM | 2011年 / 6卷 / 06期

关键词：

benzotriazoles; inhibitors; metabolic disorders; PTP1B; TCPTP; TYROSINE-PHOSPHATASE; 1B; STRUCTURE-BASED DESIGN; INSULIN-RESISTANCE; STRUCTURAL BASIS; ACID; SENSITIVITY; GLYCEMIA; OBESITY;

D O I：

10.1002/cmdc.201100077

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A two-hand grasp on one enzyme: A novel series of dual-site benzotriazole derivatives are reported as potent PTP1B inhibitors. Some of the test compounds exhibit good selectivity for PTP1B over various other PTPs, including TCPTP (invitro), and the lead compound 10h shows excellent antidiabetic activity (invivo). © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：1011 / 1016

页数：6

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