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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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| Published in: | ChemMedChem 2011-06, Vol.6 (6), p.1011-1016 |
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| Main Authors: | , , , , , , , , , , , , , |
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| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c4487-1249ee6516ab2880c6ef9ddc993812aeec09e305f767ef0a76f79ce993e5c2ed3 |
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| cites | cdi_FETCH-LOGICAL-c4487-1249ee6516ab2880c6ef9ddc993812aeec09e305f767ef0a76f79ce993e5c2ed3 |
| container_end_page | 1016 |
| container_issue | 6 |
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| container_title | ChemMedChem |
| container_volume | 6 |
| creator | 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 |
| description | 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). |
| doi_str_mv | 10.1002/cmdc.201100077 |
| format | article |
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| fulltext | fulltext |
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| source | Wiley |
| 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 |
| title | Discovery of Orally Active, Potent, and Selective Benzotriazole-Based PTP1B Inhibitors |
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