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标题：QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS BETWEEN HYDROXAMIC ACIDS AND THEIR UREASE INHIBITORY POTENCY
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作者：KEIICHI MUNAKATA ; KYOICHI KOBASHI ; JUNICHI HASE 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1980
卷号：3
期号：9
页码：457-462
DOI：10.1248/bpb1978.3.457
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：indicator variable