Synthesis and antidiabetic activity of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines and thieno[2,3-b]pyridines
| Autor: | Honey Modi, Mukul R. Jain, Pankaj R. Patel, Arun A. Gupta, Rajesh H. Bahekar, Dipam Patel, Ajay Sharma, Pradip Jadav, Vijay M. Prajapati, Debdutta Bandyopadhya, Robby Tom |
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| Rok vydání: | 2007 |
| Předmět: |
Blood Glucose
Male Stereochemistry Ratón Pyridines Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Mice In vivo Drug Discovery Insulin Secretion Animals Hypoglycemic Agents Insulin Insulin secretion Molecular Biology Bicyclic molecule Chemistry Organic Chemistry In vitro Mice Inbred C57BL Concentration dependent Molecular Medicine Cell based |
| Zdroj: | Bioorganicmedicinal chemistry. 15(21) |
| ISSN: | 0968-0896 |
| Popis: | In the present investigation, two series of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines (2a–l) and thieno[2,3-b]pyridines (3a–l) were designed as analogs of BL 11282 (1). The in vitro glucose dependent insulinotropic activity of all the test compounds was evaluated using RIN5F cell based assay and all the test compounds showed glucose and concentration dependent insulin secretion. The in vivo antidiabetic activities of most potent compounds from each series (2c and 3c) were assessed in C57BL/6J mice. Compounds 2c and 3c showed dose dependent insulin secretion and significant glucose reduction in vivo. In general, compounds 2c and 3c were found to be equipotent at all the three different doses selected and with respect to BL 11282, both the test compounds were found to be more potent, at all the time points. |
| Databáze: | OpenAIRE |
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