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

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 (in vitro), and the lead compound 10 h shows excellent antidiabetic ac...

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Bibliographic Details
Published in:ChemMedChem 2011-06, Vol.6 (6), p.1011-1016
Main Authors: Patel, Dipam, Jain, Mukul, Shah, Shailesh R., Bahekar, Rajesh, Jadav, Pradip, Darji, Brijesh, Siriki, Yernaidu, Bandyopadhyay, Debdutta, Joharapurkar, Amit, Kshirsagar, Samadhan, Patel, Harilal, Shaikh, Mubeen, Sairam, Kalapatapu V. V. M., Patel, Pankaj
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
benzotriazoles
Diabetes Mellitus - drug therapy
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacokinetics
Enzyme Inhibitors - pharmacology
Enzyme Inhibitors - therapeutic use
Humans
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacokinetics
Hypoglycemic Agents - pharmacology
Hypoglycemic Agents - therapeutic use
inhibitors
Male
metabolic disorders
Mice
Mice, Inbred C57BL
Models, Molecular
Protein Binding
Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors
Protein Tyrosine Phosphatase, Non-Receptor Type 1 - metabolism
PTP1B
Rats
Rats, Wistar
Structure-Activity Relationship
TCPTP
Triazoles - chemistry
Triazoles - pharmacokinetics
Triazoles - pharmacology
Triazoles - therapeutic use
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Summary: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 (in vitro), and the lead compound 10 h shows excellent antidiabetic activity (in vivo).
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201100077