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

共 50 条

[21] The design strategy of selective PTP1B inhibitors over TCPTP
Li, XiangQian
Wang, LiJun
Shi, DaYong
BIOORGANIC & MEDICINAL CHEMISTRY, 2016, 24 (16) : 3343 - 3352
[22] Identification of novel, active-site inhibitors of PTP1b
Zhang, YL
Xu, WX
Wan, ZK
Kirincich, SJ
Wilson, D
Follows, B
Markus, M
Tam, M
Tam, S
Tobin, JF
Lee, JB
Erbe, DV
DIABETES, 2005, 54 : A502 - A503
[23] Polycyclic phloroglucinols as PTP1B inhibitors from Hypericum longistylum: Structures, PTP1B inhibitory activities, and interactions with PTP1B
Cao, Xiangrong
Yang, Xueyuan
Wang, Peixia
Liang, Yue
Liu, Feng
Tuerhong, Muhetaer
Jin, Da-Qing
Xu, Jing
Lee, Dongho
Ohizumi, Yasushi
Guo, Yuanqiang
BIOORGANIC CHEMISTRY, 2017, 75 : 139 - 148
[24] Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors
Giroux, Andre
Boulet, Louise
Brideau, Christine
Chau, Anh
Claveau, David
Cote, Bernard
Ethier, Diane
Frenette, Richard
Gagnon, Marc
Guay, Jocelyne
Guiral, Sebastien
Mancini, Joseph
Martins, Evelyn
Masse, Frederic
Methot, Nathalie
Riendeau, Denis
Rubin, Joel
Xu, Daigen
Yu, Hongping
Ducharme, Yves
Friesen, Richard W.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (20) : 5837 - 5841
[25] Crystal structure of PTP1B complexed with a potent and selective bidentate inhibitor
Sun, JP
Fedorov, AA
Lee, SY
Guo, XL
Shen, K
Lawrence, DS
Almo, SC
Zhang, ZY
JOURNAL OF BIOLOGICAL CHEMISTRY, 2003, 278 (14) : 12406 - 12414
[26] Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors
Pinard, Emmanuel
Alberati, Daniela
Bender, Markus
Borroni, Edilio
Brom, Virginie
Burner, Serge
Fischer, Holger
Hainzl, Dominik
Halm, Remy
Hauser, Nicole
Jolidon, Synese
Lengyel, Judith
Marty, Hans-Peter
Meyer, Thierry
Moreau, Jean-Luc
Mory, Roland
Narquizian, Robert
Norcross, Roger D.
Schmid, Philipp
Wermuth, Roger
Zimmerli, Daniel
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (23) : 6960 - 6965
[27] Discovery of potent and selective orally active inhibitors of anaplastic lymphoma kinase (ALK)
Shakespeare, William
Fantin, Valeria
Wang, Frank
Kohlmann, Anna
Liu, Shuangying
Huang, Wei-Sheng
Wang, Yihan
Zou, Dong
Thomas, Mathew
Li, Feng
Qi, Jiwei
Cai, Lisi
Dwight, Thimothy
Xu, Yongjin
Xu, Rongsong
Dodd, Rory
Xu, Qihong
Anjum, Rana
Zhang, Sen
Keats, Jeffrey
Xue, Ling
Wardwell, Scott
Ning, Yaoyu
Moran, Lauren
Mohemmad, Qurish
Zhu, Xiaotian
Narasimhan, Narayana
Rivera, Victor
Dalgarno, David
Clackson, Tim
CANCER RESEARCH, 2009, 69
[28] Discovery of triazines as potent, selective and orally active PDE4 inhibitors
Gewald, Rainer
Grunwald, Christian
Egerland, Ute
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (15) : 4308 - 4314
[29] Discovery of potent PTP1B inhibitors via structure-based drug design, synthesis and in vitro bioassay of Norathyriol derivatives
Xue, Wenjie
Tian, Jinlong
Wang, Xiang Simon
Xia, Jie
Wu, Song
BIOORGANIC CHEMISTRY, 2019, 86 : 224 - 234
[30] Discovery of novel high potent and cellular active ADC type PTP1B inhibitors with selectivity over TC-PTP via modification interacting with C site
Du, Yongli
Zhang, Yanhui
Ling, Hao
Li, Qunyi
Shen, Jingkang
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 144 : 692 - 700

← 1 2 3 4 5 →