• The Korean Journal of Pesticide Science
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• v.8 no.2
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• pp.79-87
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• 2004

3-Chloro-2-[4-chloro-2-fluoro-5-(5-methyl-3-phenyl-4,5-dihydroisoxazol-5-ylmethoxy)-phenyl]-4,5,6,7-tetrahy dro-2H-indazole(EK-5439) demonstrated rice selectivity and herbicidal activity on annual weeds, such as Echinochloa oryzicola, Monochoria vaginalis, Lindernia pyxidaria, Rotala indica, Aneilema keisak, Cyperus difformis, and Ludwigia prostrata at doses of 16-63 g a.i./ha. However, the application window was limited from pre-emergence to 5 days after transplanting. The control efficacy of EK-5439 on barnyardgrass was 4 times higher than that of oxadiazon. EK-5439 was excellently safe to the 16 different transplanted rice cultivars treated 2 days after transplanting. These compounds have the mechanism of action on the chlorophyll biosynthesis like protoporphyrinogen IX oxidase inhibitors.

• Korean Journal of Weed Science
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• v.7 no.2
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• pp.220-235
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• 1987

The experiment was carried out to find the feasibility of using Oxyfluorfen in the paddy fields by investigating the difference of selective activity of Oxyfluorfen among rice cultivars and major paddy weed species. The dosage of Oxyfluorfen that show selective activity between rice cultivars and weed species ranged from 0.1 to 0.4kg ai/ha. The degree of growth inhibition was in order of whole-plant soaking application > root soaking application > stem bandage application, and in that case $10^{-5}$M Oxyfluorfen was treated after emergence. Especially the growth inhibition of rice cultivars and Cyperus serotinus was low, among others. Photosynthesis was severely inhibited at the Oxyfluorfen level above $10^{-4}$ M in all the tested weeds, but inhibition of respiration was not to be seen. Isolated single cells of two rice cultivars and Cyperus serotinus were tolerant to $10^{-5}$M Oxyfluorfen,but those of Echinochloa crus-galli and Sagittaria pygmaea were susceptible comparatively. The growth inhibition of suspension cultured rice cell induced by the increments of Oxyfluorfen concentration, and the degree of inhibition was higher in C.V. Mushakdanti than in C.V. Aichiasahi.

• The Korean Journal of Pesticide Science
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• v.5 no.3
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• pp.1-11
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• 2001

New technologies will have a large impact on the discovery of new herbicide site of action. Genomics, combinatorial chemistry, and bioinformatics help take advantage of serendipity through tile sequencing of huge numbers of genes or the synthesis of large numbers of chemical compounds. There are approximately $10^{30}\;to\;10^{50}$ possible molecules in molecular space of which only a fraction have been synthesized. Combining this potential with having access to 50,000 plant genes in the future elevates tile probability of discovering flew herbicidal site of actions. If 0.1, 1.0 or 10% of total genes in a typical plant are valid for herbicide target, a plant with 50,000 genes would provide about 50, 500, and 5,000 targets, respectively. However, only 11 herbicide targets have been identified and commercialized. The successful design of novel herbicides depends on careful consideration of a number of factors including target enzyme selections and validations, inhibitor designs, and the metabolic fates. Biochemical information can be used to identify enzymes which produce lethal phenotypes. The identification of a lethal target site is an important step to this approach. An examination of the characteristics of known targets provides of crucial insight as to the definition of a lethal target. Recently, antisense RNA suppression of an enzyme translation has been used to determine the genes required for toxicity and offers a strategy for identifying lethal target sites. After the identification of a lethal target, detailed knowledge such as the enzyme kinetics and the protein structure may be used to design potent inhibitors. Various types of inhibitors may be designed for a given enzyme. Strategies for the selection of new enzyme targets giving the desired physiological response upon partial inhibition include identification of chemical leads, lethal mutants and the use of antisense technology. Enzyme inhibitors having agrochemical utility can be categorized into six major groups: ground-state analogues, group specific reagents, affinity labels, suicide substrates, reaction intermediate analogues, and extraneous site inhibitors. In this review, examples of each category, and their advantages and disadvantages, will be discussed. The target identification and construction of a potent inhibitor, in itself, may not lead to develop an effective herbicide. The desired in vivo activity, uptake and translocation, and metabolism of the inhibitor should be studied in detail to assess the full potential of the target. Strategies for delivery of the compound to the target enzyme and avoidance of premature detoxification may include a proherbicidal approach, especially when inhibitors are highly charged or when selective detoxification or activation can be exploited. Utilization of differences in detoxification or activation between weeds and crops may lead to enhance selectivity. Without a full appreciation of each of these facets of herbicide design, the chances for success with the target or enzyme-driven approach are reduced.

• Applied Biological Chemistry
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• v.47 no.4
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• pp.414-421
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• 2004

3D QSAR studies for protox inhibition activities against root and shoot of the rice plant (Orysa sativa L.) and barnyardgrass (Echinochloa crus-galli) by a series of new 1-(5-methyl-3-phenylisoxazolin-5-yl)methoxy-2-chloro-4-fluorobenzene derivatives were conducted based on the results (Sung, N. D. et al.'s, (2004) J. Korean Soc. Appl. Biol. Chem. 47(3), 351-356) using comparative molecular similarity indices analysis (CoMSIA) methodology. Four CoMSIA models, without hydrogen bond donor field for the protox inhibition activities against root and shoot of the two plants, were derived from the combination of several fields using steric field, hydrophobic field, hydrogen bond acceptor field, LUMO molecular orbital field, dipole moment (DM) and molar refractivity (MR) as additional descriptors. The predictabilities and fitness of CoMSIA models for protox inhibition activities against barnyard-grass were higher than that of rice plant. The statistical results of these models showed the best predictability of the protox inhibition activities against barnyard-grass based on the cross-validated value $r^2\;_{cv}\;(q^2=0.635{\sim}0.924)$, non cross-validated, conventional coefficient $r^2\;_{ncv.}$ value $(r^2=0.928{\sim}0.977)$ and PRESS value $(0.255{\sim}0.273)$. The protox inhibition activities exhibited a strong correlation with the steric $(5.4{\sim}15.7%)$ and hydrophobic $(68.0{\sim}84.3%)$ factors of the molecules. Particularly, the CoMSIA models indicated that the groups of increasing steric bulk at ortho-position on the C-phenyl ring will enhance the protox inhibition activities against barnyard-grass and subsequently increase the selectivity.