Quantitative structure-activity relationships between hydroxamic acids and their urease inhibitory potency
| Autor: | Keiichi Munakata, Kyoichi Kobashi, Jun'ichi Hase |
|---|---|
| Rok vydání: | 1980 |
| Předmět: |
Pharmacology
Steric effects Quantitative structure–activity relationship Hydroxamic acid Chemical Phenomena Urease biology Chemistry Physical Stereochemistry Quantitative structure Hydroxamic Acids Structure-Activity Relationship Inhibitory potency chemistry.chemical_compound chemistry biology.protein Moiety |
| Zdroj: | Journal of Pharmacobio-Dynamics. 3:457-462 |
| ISSN: | 1881-1353 0386-846X |
| Popis: | Quantitative structure activity relationships between physico-chemical properties of four series of more than sixty hydroxamic acids [R-(CONHCH2)n-CONHOH, R=aromatic or aliphatic, n=1 or 0) and their urease inhibitory activities were examined. The best improved regression equation equation primarily indicated that the inhibitory activities of hydroxamic acids were parabolically varied with the hydrophobic variable, π of the R moiety and the optimal π value was calculated to be 2.58. Furthermore, the inhibitory activities of congeners were found to be significantly affected by the B1 variable representing the minimum width of steric size of the R moiety. Besides, it was clarified by using two indicator variables that inhibitory activities were not affected by the R moiety, whether aromatic or aliphatic, but positively affected by the presence of the -CONHCH2-group between the R moiety and the hydroxamic acid group. |
| Databáze: | OpenAIRE |
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