88093-48-5Relevant academic research and scientific papers
Design, synthesis, and bioactivities of novel pyridazinone derivatives containing 2-phenylthiazole or oxazole skeletons
Dang, Mingming,Liu, Minhua,Huang, Lu,Ou, Xiaoming,Long, Chuyun,Liu, Xingping,Ren, Yeguo,Zhang, Ping,Huang, Mingzhi,Liu, Aiping
, p. 4088 - 4098 (2020/10/02)
A series of novel pyridazinone derivatives were designed and synthesized by replacing 4-(tert-butyl)phenyl moiety of pyridaben with 2-phenylthiazole or oxazole fragments via activity substructure connecting approach. The structures of all target compounds were characterized through NMR, MS, and elemental analysis. Bioassay results exhibit that most compounds showed potent bioactivities against Aphis fabae, Tetranychus urticae, Erysiphe graminis, and/or Puccinia polysora. Among the newly synthesized compounds, 2-(tert-butyl)-4-chloro-5-(((2-phenylthiazol-4-yl)methyl)thio)pyridazin-3(2H)-one (12b) displays remarkable insecticidal activity against A fabae. Its LC50 value (2.73 mg/L) is better than that of pyridaben (5.46 mg/L), although inferior to that of imidacloprid (0.51 mg/L). In addition to its extraordinary insecticidal activity, compound 12b also exerts 96.9% fungicidal activities against P polysora at 500 mg/L in vivo, significantly superior to that of pyridaben (50.0%), while slightly lower than that of tebuconazole (100%). This article discusses the synthesis, bioassay results, and structure-activity relationship of this series of novel pyridazinone derivatives.
DIAGNOSTIC AGENT FOR THERAPEUTIC EFFECT ON CANCER
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Paragraph 0075; 0076; 0077, (2016/09/26)
The present invention provides a diagnostic agent for a therapeutic effect on cancer, containing a compound represented by formula (1-0). (In formula (1-0), R represents —O(CH2)n—, —O(CH2)nOC2H4—, —CH2O(CH2)n—, or —CH2O(CH2)nOC2H4—, n represents an integer of 1 to 5, and Q1 represents F or —OCH3.)
Pyridazinone derivative, and preparation method and application thereof
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Paragraph 0017, (2016/11/02)
The invention relates to a pyridazinone derivative with the structure shown in the description. R1 and R2 groups in the structure are selected from specific groups in the description. The invention discloses the structure of the compound, and an agriculture pest prevention and control effect of the compound, and also discloses an application of the compound as a pesticide.
COMPOUND SUITABLE FOR DETECTION OF MITOCHONDRIAL COMPLEX-1
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Paragraph 0063; 0064; 0065, (2015/09/22)
Provided is a compound represented by formula (1-0): wherein in formula (1-0), R represents —O(CH2)n—, —O(CH2)nOC2H4—, —CH2O(CH2)n— or —CH2O(CHs
Development of novel PET probes, [18F]BCPP-EF, [ 18F]BCPP-BF, and [11C]BCPP-EM for mitochondrial complex 1 imaging in the living brain
Harada, Norihiro,Nishiyama, Shingo,Kanazawa, Masakatsu,Tsukada, Hideo
, p. 553 - 561 (2013/11/06)
We developed three novel positron-emission tomography (PET) probes, 2-tert-butyl-4-chloro-5-{6-[2-(2[18F]fluoroethoxy)-ethoxy]-pyridin-3- ylmethoxy}-2H-pyridazin-3-one ([18F]BCPP-EF), 2-tert-butyl-4-chloro- 5-[6-(4-[18F]fluorobutoxy)-pyridin-3-ylmethoxy]-2H-pyridazin-3-one ([18F]BCPP-BF), and 2-tert-butyl-4-chloro-5-{6-[2-(2-[ 11C]methoxy-ethoxy)-ethoxy]-pyridin-3-ylmethoxy}-2H-pyridazin-3-one ([11C]BCPP-EM), for quantitative imaging of mitochondrial complex 1 (MC-1) activity in vivo. These three PET probes were successfully labeled by nucleophilic [18F]fluorination or by [11C]methylation of their corresponding precursor with sufficient radioactivity yield, good radiochemical purity, and sufficiently high specific radioactivity for PET measurement. The specificity of these probes for binding to MC-1 was assessed with rotenone, a specific MC-1 inhibitor, by a rat brain slice imaging method in vitro. Rat whole-body imaging by small-animal PET demonstrated that all probes showed high uptake levels in the brain as well as in the heart sufficient to image them clearly. The rank order of uptake levels in the brain and the heart just after injection was as follows: high in [18F]BCPP-BF, intermediate in [11C]BCPP-EM, and low in [18F]BCPP-EF. The kinetics of [18F]BCPP-EF and [11C]BCPP-EM provided a reversible binding pattern, whereas [18F]BCPP-BF showed nonreversible accumulation-type kinetics in the brain and heart. Metabolite analyses indicated that these three compounds were rapidly metabolized in the plasma but relatively stable in the rat brain up to 60 min post-injection. The present study demonstrated that [18F]BCPP-EF could be a useful PET probe for quantitative imaging of MC-1 activity in the living brain by PET. Copyright
METHODS AND APPARATUS FOR SYNTHESIZING IMAGING AGENTS, AND INTERMEDIATES THEREOF
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Page/Page column 155, (2011/09/14)
The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comp
Synthesis and antifeedant activity of new oxadiazolyl 3(2H)-pyridazinones
Cao, Song,Qian, Xuhong,Song, Gonghua,Chai, Bing,Jiang, Zhisheng
, p. 152 - 155 (2007/10/03)
A total of 20 new compounds containing the oxadiazolyl 3(2H)-pyridazinone moiety were synthesized. The structures of all the compounds were confirmed by 1H NMR, IR, MS, and elemental analysis. Their insect antifeedant activities against Asiatic corn borer Ostrinia furnacalis (Guenee) were examined and compared with commercial azadirachtin. The compounds exhibited significant levels of activity. The feeding deterrency values of IIIa,j were 57% and 51% at 500 mg/kg concentration, respectively.
