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Hirokazu Osabe Yasuo Morishima Yukihisa Goto Kazuhisa Masamoto Yoshiaki Nakagawa Toshio Fujita 《Pest management science》1992,34(1):27-36
The variations in the light-dependent herbicidal activity against Echinochloa oryzicola of a number of 4-pyridone-3-carboxanilides with various substituents on the anilide and pyridone rings have been examined by use of physicochemical substituent parameters and regression analysis. The effects of substituents of the anilide ring were such that the activity was related parabolically not only with the substituent hydrophobicity (π) but also with the steric bulk parameter (Es) of the bulkier ortho substituent. The effect of substituents at the 1-position of the pyridone ring was analysed with steric(STERIMOL L and B5) and electronic(γ1) parameters. That of substituents at the 5-position of the pyridone ring was explained by a parabolic function of a steric (MR) parameter. Analyses of the activity of 105 analogs confirmed that our previous selection of a candidate compound in this series for field trials was indeed appropriate in terms of physicochemical substituent effects. 相似文献
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Hirokazu Osabe Yasuo Morishima Yukihisa Goto Kazuhisa Masamoto Yoshiaki Nakagawa Toshio Fujita 《Pest management science》1992,34(1):17-25
A number of substituted 4-pyridone-3-carboxanilide derivatives show various degrees of light-dependent herbicidal activity. The effects of substituents at the anilide moiety on the activity against Echinochloa oryzicola were analysed quantitatively with physicochemical substituent parameters. The activity was shown to vary parabolically with total hydrophobicity (Σπ) of the anilide ring substituents as well as with the steric parameter (Es) of the ortho-substituents. The Es parameter for only the bulkier ortho-substituent, with the more negative value, but not for the two, was significant. The effect of substituents at the 1-position was expressible by indicator variables assigned to each 1-substituted series, the physicochemical rationalization being left for future analyses. 相似文献
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Hirokazu Osabe Yasuo Morishima Yukihisa Goto Toshio Fujita 《Pest management science》1992,35(2):187-200
Using a set of representative members selected from 4-pyridone-3-carboxanilides and ortho-chlorinated diphenyl ethers exhibiting light-dependent herbicidal activity, we examined the three-dimensional structure-activity relationships quantitatively. The most stable conformation of each compound, regarded as the ‘active conformation’, was determined by either semi-empirical or ab initio molecular orbital calculations. With a hypothesis defining a common substructural skeleton between the two different compound series. each molecule was superimposed. We first analysed the structure-activity relationship using an index for the substructure shape similarity according to the superimposed conformations. After finding the relevance of the hypothesis, we examined the three-dimensional structure-activity relationship using the comparative molecular field analysis procedure. The results suggested that the two different series of compounds have a common region of the receptor site. The variations in the light-dependent herbicidal potency were governed by hydrophobicty and three-dimensional steric and electronic field parameters of molecules participating in the transport process and the interaction with the receptor site. The result was consistent with that derived from our previous quantitative analysis with the use of free-energy-related substituent parameters and the traditional regression procedure for a large number of pyridone-carboxanilides. 相似文献
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Protein binding kinetics of lincomycin (LM) and clindamycin (CM) were studied using plasma, albumin and α1-acid glycoprotein (AGP) derived from humans, dogs, cattle and sheep. Based on Rosenthal plots of LM and CM, drug-binding property in plasma presented specific and non-specific binding, except for LM in cattle and sheep and for CM in sheep, where only non-specific binding was demonstrated. Dissociation constant (Kd) and binding capacity (Bmax) for specific binding and proportionality constant (PC) for non-specific binding were as follows: Kd = 3.14 μmol/L, Bmax = 15.28 μmol/L, PC = 0.19 for humans; Kd = 3.84 μmol/L, Bmax = 6.55 μmol/L, PC = 0.14 for dogs; PC = 0.12 for cattle; PC = 0.16 for sheep in LM and Kd = 0.94 μmol/L, Bmax = 12.24 μmol/L, PC = 4.98 for humans; Kd = 1.48 μmol/L, Bmax = 9.52 μmol/L, PC = 2.91 for dogs; Kd = 1.22 μmol/L, Bmax = 4.45 μmol/L, PC = 2.40 for cattle; PC = 1.48 for sheep in CM. The specific binding for each species was different, showing more difference in Bmax compared with Kd. The non-specific binding of LM was similar among species whereas that of CM was different, implying species difference. The drug-binding property of AGP for each species was all specific binding and the Kd was comparable to that obtained from plasma, indicating that AGP is a major specific binder in plasma. The lack of detection of specific binding for LM in cattle and sheep and for CM in sheep plasma could be attributable to a higher Kd and lower plasma AGP concentration compared with other species. The drug-binding property of albumin was characterized as all non-specific, without a great difference among species. Except for CM in sheep, the lower PC in albumin solution compared with that in plasma suggested the presence of another non-specific binder in plasma, i.e. lipoprotein. From the simulation of drug-binding percentage to AGP concentrations, AGP could be a major contributor to drug-plasma protein binding in pathological states. The degree of AGP-drug binding for each species could vary according to the degree of increase of AGP concentrations from a healthy to a pathological state, inducing a decrease in the unbound fraction (fp): 6.1 fold for dogs, 4.6 fold for humans, 1.8 fold for sheep and 1.4 fold for cattle in LM; 5.8 fold for dogs, 5.7 fold for cattle, 4.0 fold for humans and 1.5 fold for sheep in CM. Therefore, the disposition and efficacy of lincosamides affected by fp can be modified differently by the change of fp attributable to the alteration of plasma AGP concentration in each species. 相似文献
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Kazutaka Kawamura Motoki Shimizu Takahiro Kawanabe Zujing Pu Taro Kodama Makoto Kaji Kenji Osabe Ryo Fujimoto Keiichi Okazaki 《Euphytica》2017,213(1):28
Cabbage (Brassica oleracea L. var. capitata) is an important vegetable worldwide. Most Japanese commercial cultivars of cabbage use an F1 hybrid seed production system. The purity of F1 hybrid seeds is important and the assessment of purity based on DNA markers can be highly accurate. In addition, selection of agronomically important traits such as disease resistance based on DNA markers is useful for breeding of cabbage. The aim of this study is to demonstrate the effectiveness of DNA marker-assisted selection in cabbage. In this study we distinguished the parental S haplotypes in 35 F1 hybrid cultivars by combining several linked DNA markers. Thirty-one highly polymorphic simple sequence repeats (SSR) markers were screened from 175 reported SSR markers, which are useful for assessment of the purity of F1 hybrid seeds. We examined the relationship between the DNA marker based genotype and the phenotype by an inoculation test of clubroot disease. A co-dominant PCR–RFLP marker was developed for selection of Fusarium yellows resistance and the genotypes using this marker were consistent with inoculation test in all tested samples. 相似文献
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