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

[41] Identification of natural products as selective PTP1B inhibitors via virtual screening
Yang, Ying
Tian, Jin-Ying
Ye, Fei
Xiao, Zhiyan
BIOORGANIC CHEMISTRY, 2020, 98
[42] Small Molecule Inhibitors of PTP1B and TCPTP
Reddy, M. V. V. V. Sekhar
Chakshusmathi, G.
Narasu, M. Lakshmi
INTERNATIONAL JOURNAL OF PHARMACEUTICAL AND PHYTOPHARMACOLOGICAL RESEARCH, 2012, 1 (05): : 287 - 291
[43] PTP1B inhibitors from Ardisia japonica
Li, YF
Hu, LH
Lou, FC
Li, J
Shen, Q
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH, 2005, 7 (01) : 13 - 18
[44] Integrated Approach to Identify Selective PTP1B Inhibitors Targeting the Allosteric Site
Yang, Ying
Zhang, Lei
Tian, Jinying
Ye, Fei
Xiao, Zhiyan
JOURNAL OF CHEMICAL INFORMATION AND MODELING, 2021, 61 (09) : 4720 - 4732
[45] Discovery of orally active selective inhibitors of Plk1[p]
Pinder, Joanne L.
Durrant, Steven
Everitt, Simon
Mortimore, Michael
Keily, Shazia
Knegtel, Ronald
O'Donnell, Michael
Brenchley, Guy
Charrier, Jean-Damien
Golec, Julian
Kay, David
Mak, Chau
Ramaya, Sharn
Rutherford, Alistair
Studley, John
Virani, Anisa
Weber, Peter
Young, Stephen C.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2012, 243
[46] A potent, selective, and orally bioavailable inhibitor of the protein-tyrosine phosphatase PTP1B improves insulin and leptin signaling in animal models
Krishnan, Navasona
Konidaris, Konstantis F.
Gasser, Gilles
Tonks, Nicholas K.
JOURNAL OF BIOLOGICAL CHEMISTRY, 2018, 293 (05) : 1517 - 1525
[47] Discovery and structural modification of novel inhibitors of PTP1B inspired by the ACT fragment of scleritodermin A
Wei, Yi
Chen, Yue-Ting
Shi, Lei
Gao, Li-Xin
Liu, Shen
Cui, Yong-Mei
Zhang, Wei
Shen, Qiang
Li, Jia
Nan, Fa-Jun
MEDCHEMCOMM, 2011, 2 (11) : 1104 - 1109
[48] Discovery of novel PTP1b inhibitors from a non-HTS hit.
Kirincich, S
Follows, B
Moretto, A
Wan, ZK
Wilson, DP
Smith, MJ
Erbe, D
Tobin, J
Zhang, YL
Tam, M
Xu, WX
Joseph-McCarthy, D
Foreman, K
Tam, S
Lee, J
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U218 - U218
[49] Discovery of potent and orally active farnesyltransferase (FT) inhibitors.
Tong, YS
Wang, L
Hasvold, L
Leonard, N
Li, TM
Li, Q
Wang, WB
Cohen, J
Gu, WZ
Zhang, HY
Bauch, J
Marsh, K
Rosenberg, SH
Lin, NH
Sham, HL
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 224 : U29 - U29
[50] The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia
Ho, Ginny D.
Yang, Shu-Wei
Smotryski, Jennifer
Bercovici, Ana
Nechuta, Terry
Smith, Elizabeth M.
McElroy, William
Tan, Zheng
Tulshian, Deen
McKittrick, Brian
Greenlee, William J.
Hruza, Alan
Xiao, Li
Rindgen, Diane
Mullins, Deborra
Guzzi, Mario
Zhang, Xiaoping
Bleickardt, Carina
Hodgson, Robert
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (02) : 1019 - 1022

← 1 2 3 4 5 →