http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
식물 치사관련 유전자를 이용하는 신규 제초제 작용점 탐색 및 조절물질 개발동향
황인택(Hwang L.T.),이동희(D.H. Lee),최정섭(J.S. Choi),김태준(T.J. Kim),김범태(B.T. Kim),박유신(Y.S. Park),조광연(K.Y. Cho) 한국농약과학회 2001 농약과학회지 Vol.5 No.3
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 the sequencing of huge numbers of genes or the synthesis of large numbers of chemical compounds. There are approximately 10³? to 10?? 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 the probability of discovering new 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 teclmology. 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.
1,3-Dioxolan-2-yliden 유도체들의 합성과 항진균 활성
김영섭(Y. S. Kim),김우정(W. J. Kim),김범태(B. T. Kim),박노균(N. K. Park),박창식(C. S. Pak) 대한약학회 1999 약학회지 Vol.43 No.5
(1H-1,2,4-Triazolyl) methyl-4-(sub.) phenyl-5-methyl-1,3-dioxolan-2-yliden (3) derivatives were synthesized and tested for their antifungal activities. The designed compounds with a 1,2,4-triazolyl-methyl group at the 4-position of 1,3-dioxolan-2-yliden moiety were synthesized by reaction of difluorinated olefins (2) with (2R,3R)-2-(2,4-dihalophenyl)-1-(1H-1,2,4-triazol-1-yl)butane-2,3-diol (1). These compounds were tested for in vitro antifungal activities against 16 fungi species. The MIC values were determined by the micro broth dilution method. In general, 1,3-dioxolan-2-[1-(3,4-methylenedioxyphenyl) methylidene)-1,3-dioxolon-4-yl(1H-1,2,4-triazol1yl)methane showed superior antifungal activities to fluconazol and ketoconazol.