Source:http://linkedlifedata.com/resource/pubmed/id/19954223
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2010-3-3
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pubmed:abstractText |
Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) has been identified as one of the most significant action targets for a large chemically diverse family of herbicides that exhibit some interesting characteristics, such as low use rate, low toxicity to mammals, and low environmental impact. As a continuation of research work on the development of new PPO inhibitors, some benzothiazole analogues of oxadiargyl, an important PPO-inhibiting commercial herbicide, were designed and synthesized by ring-closing of the substituents at the C-4 and C-5 positions. The bioassay results indicated that the series 8, 9, and 10 have good PPO inhibition activity with k(i) values ranging from 0.25 to 18.63 microM. Most interestingly, 9l, ethyl 2-((5-(5-tert-butyl-2-oxo-1,3,4-oxadiazol-2(3H)-yl)-6-fluorobenzothiazol-2-yl)sulfanyl) propanoate, was identified as the most promising candidate due to its high PPO inhibition effect (k(i) = 1.42 microM) and broad spectrum postemergence herbicidal activity at the concentration of 37.5 g of ai/ha.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/5-tert-butyl-3-(2,4-dichloro-5-propa...,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Oxadiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Protoporphyrinogen Oxidase
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1520-5118
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
10
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pubmed:volume |
58
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2643-51
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pubmed:meshHeading |
pubmed-meshheading:19954223-Biological Assay,
pubmed-meshheading:19954223-Enzyme Inhibitors,
pubmed-meshheading:19954223-Magnetic Resonance Spectroscopy,
pubmed-meshheading:19954223-Oxadiazoles,
pubmed-meshheading:19954223-Protoporphyrinogen Oxidase,
pubmed-meshheading:19954223-Quantitative Structure-Activity Relationship,
pubmed-meshheading:19954223-Spectrometry, Mass, Electrospray Ionization
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pubmed:year |
2010
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pubmed:articleTitle |
Design, synthesis, and 3D-QSAR analysis of novel 1,3,4-oxadiazol-2(3H)-ones as protoporphyrinogen oxidase inhibitors.
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pubmed:affiliation |
Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, People's Republic of China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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