QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS BETWEEN HYDROXAMIC ACIDS AND THEIR UREASE INHIBITORY POTENCY

概要

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Quantitative structure activity relationships between physico-chemical properties of four series of more than sixty hydroxamic acids [R-(CONHCH_2)_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 B_1 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 -CONHCH_2-group between the R moiety and the hydroxamic acid group.
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