• Title/Summary/Keyword: N-Substituted-5-chloro-1,3-dimethylpyrazole-4-carboxamide

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Synthesis and antifungal activity of N-substituted-5-chloro-1,3-dimethylpyra-zole-4-carboxamide (N-치환-5-chloro-1,3-dimethylpyrazole-4-carboxamide의 합성과 살균력)

  • Kim, Yong-Whan;Jeon, Won-Bae;Park, Chang-Kyu
    • Applied Biological Chemistry
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    • v.35 no.2
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    • pp.87-91
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    • 1992
  • Twenty-six N-substituted-5-chloro-1,3-dimethylpyrazole-4-carboxamide were synthesized and their antifungal activity against Rhizoctonia solani, Pyricularia oryzae, Botrytis cinerea and Colletotricum gleosporiodes was compared. N-phenyl-5-chloro-l,3-dimethylpyrazole-4-carboxamides having electron releasing group at the meta position of phenyl ring demonstrated good fugicidal activity against R. solani.

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Quantitative structure-activity relationship of N-substituted phenyl 5-chloro-1,3-dimethylpyrazol-4-carboxamides (N-치환 phenyl 5-chloro-1,3-dimethylpyrazole-4-carboxamide의 정량적구조활성상관관계)

  • Kim, Yong-Whan;Park, Chang-Kyu
    • Applied Biological Chemistry
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    • v.35 no.5
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    • pp.382-388
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    • 1992
  • Mycelial growth inhibition activity of forty-one N-substituted phenyl 5-chloro-1,3-dimethylpyrazole-4-carboxamides against Rhizoctonia solani was analysed quantitatively by multiple regression analysis using physicochemical parameters of substituents as independent variables and $pEC_{50}$ as dependent variable. As a result, a quantitative structure-activity relationship was formulated using eight physicochemical parameters, which explains 83% of variance of the fungicidal activity. The most important parameter for the biological activity was log k', as related to the penetration and transport processes in the biological system. The activity also correlated with other hydrophobic parameters$({\pi}_2,\;{\pi}_3)$, an electronic parameter$({\Sigma}{\sigma})$, and steric parameters$(STERIMOL\;parameters\;L_3,\;L_4)$.

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