• Title/Summary/Keyword: Pyrazole

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Insecticidal activity of flupyrazofos KH502 against Plutella xylostella: a CoMFA study (배추좀나방에 대한 flupyrazofos KH502의 살충활성 CoMFA)

  • Kim, Soo-Kyung;Lee, Kwan-Gu;Kim, Hey-Won;Yoo, Sung-Eun;Hwang, Ki-Jun;Gong, Young-Dae
    • The Korean Journal of Pesticide Science
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    • v.8 no.3
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    • pp.162-167
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    • 2004
  • In recent years, the diamondback moth (DBM), Plutella xylostella has become one of the most important pests for cruciferous plants in the world. A new type of the thiophosphoryl pyrazole insecticide, called KH502. Its outstanding insecticidal activity could be effective alternative against DBM. We investigated, using the comparative molecular field analysis (CoMPA) method, The structure-activity relationship of various thiophosphorylpyrazole derivatives and structure requirement for insecticidal activity. We found, the key substructures in pyrazole derivatives, the trifluoro-methyl group and the thiophosphoryl group. Both play an important role in insecticidal activity with the binding site. The three dimensional Quantitative Structure Activity Relationship (QSAR) analysis could provide useful information for the structural requirements of pyrazole insecticide as an insecticidal and the design of a new insecticide.

A Facile Greener Assisted Protocol for the Synthesis of Some New 4-aryl-(5-chloro-3-Methyl-1-phenyl-1H-Pyrazol-4-yl)-4,5-dihydroisoxazol-3-yl) Derivatives and their in vitro Antimicrobial Activity

  • Shaikh, Baseer M.;Konda, Shankaraiah G.;Yemul, Omprakash S.;Dawane, Bhaskar S.
    • Journal of the Korean Chemical Society
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    • v.56 no.2
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    • pp.246-250
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    • 2012
  • An efficient access, single step and environmentally benign synthesis of a new series of pyrazole containing isoxazolines derivatives were prepared by the condensation of chalcones bearing pyrazole moiety with hydroxyl amine hydrochloride in basic condition by using polyethylene glycol-400 (PEG) as a greener reaction solvent. The advantages of the present methodology are mild reaction condition and avoidance of volatile organic solvent. Furthermore, these newly synthesized compounds were screened for their antimicrobial activity against various pathogens like Escherichia coli (MTCC 2939), Salmonella typhi (MTCC 98), Staphylococcus aureus (MTCC 96), Bacillus subtilis (MTCC 441), Aspergillus niger (MTCC 281), Aspergillus flavus (MTCC 2501), Penicillium chrsogenum (MTCC 160) and Fusarium moniliformae (MTCC 156). Especially compound containing the hydroxyl group in C2-position and presence of halo (I, Br and Cl) groups as substituents at $C_3$ and $C_5$ position on the benzene nucleus showed the higher activity. Furthermore, compounds bearing methyl groups in combination with I and Br which enhanced the activity.