A novel series of N-(1-aminoalkylidene)carboximidamides as potential hypoglycemic agents
| Autor: | Charles R. Bowden, Mary C. Rebarchak, Tuman Robert W, Henry J. Breslin, Michael J. Kukla |
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| Rok vydání: | 1993 |
| Předmět: |
Glucose tolerance test
medicine.diagnostic_test Stereochemistry Biological activity Pharmacology Glucose Tolerance Test Imides Amides Rats Amidine chemistry.chemical_compound Structure-Activity Relationship Linogliride chemistry Biological significance In vivo Drug Discovery medicine Molecular Medicine Animals Hypoglycemic Agents Clinical efficacy Antidiabetic agents |
| Zdroj: | Journal of medicinal chemistry. 36(11) |
| ISSN: | 0022-2623 |
| Popis: | Nitrogen heterocyclic carboximidamides, such as linogliride, 1a, have been shown to possess significant hypoglycemic activity and have shown clinical efficacy as potential antidiabetic agents. We evaluated the biological significance of the heterocyclic ring A of general structure 1, which has always been maintained in this class of compounds, by preparing acyclic compounds of general structure 2. Preliminary in vivo biological testing, i.e., the glucose tolerance test in rats, indicates that a number of the specific acyclic carboximidamides prepared, 6a-kk, possessed significant hypoglycemic activity often comparable to, and in some cases better than, the activity noted for our model compound, 1a. These results suggest that the heterocyclic ring A of 1 is not essential for hypoglycemic activity for this class of compounds. |
| Databáze: | OpenAIRE |
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