• Title/Summary/Keyword: carboxamides

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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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Synthesis of trifluoromethylated dihydro-1,4-dithiin carboxamides and their antifungal activities (Trifluoromethylated Dihydro-1,4-dithiin carboxanilide 유도체의 합성 및 살균활성)

  • Hahn, Hoh-Gyu;Nam, Kee-Dal;Chang, Kee-Hyuk;Lee, Seon-Woo;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
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    • v.5 no.2
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    • pp.26-32
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    • 2001

  • [ ${\alpha},{\beta}$ ]-Unsaturated carboxamides 12 with trifluromethylated dihydro-1,4-dithiins were synthesized for the purpose of development of new agrochemical fungicide. Chlorination of trifluoromethylated ${\beta}$-ketoester 4 followed by tile reaction with 1,2-ethanedithiol gave intermediate 1,4-dithiane 9. Without purification of 9 substitution of hydroxy by chlorine followed by dehydrochlorination in the presence of triethylamine afforded trifluoromethylated dihydro-1,4-dithiin ethyl ester 7. Activation of the hydroxy of the carboxylic acid 10 obtained from the hydrolysis of 7 and then reacted with various amines gave the corresponding trifluoromethylated dihydro-1,4-dithiin carboxamides. Antifungal screening (in vivo) against typical plant diseases, Rice Blast, Rice Sheath Blight, Cucumber Gray Mold, Tomato Late Blight, Wheat Leaf Rust, and Barley Powdery Mildew of the synthesized compounds was carried out. As a result, most of the compounds shlowed weak antifungal activities and some compounds in which isopropyl group was substituted in meta of the phenyl showed antifungal activity (99%) at 250 ppm against the disease Wheat Leaf Rust.

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Studies on the Anti-inflammatory Agents. Synthesis of Carboxamides and Their Anti-inflammatory Activity

  • Chae, Dong-Kyu
    • YAKHAK HOEJI
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    • v.21 no.4
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    • pp.173-176
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    • 1977

  • Four compounds, benzamide, N-(3-trifluoromethylphenyl) benzamide, N-(2,3-dimethylphenyl) cinnamamide and N-(3-trifluoromethylphenyl) cinnamamide, were synthesized and evaluated their activity by the method of the inhibitory effect on the carrageenin-induced rat paw edema, compared with phenylbutazone. All of these exhibited anti-inflammatory activity, and N-(2,3-dimethylphenyl) benzamide exhibited 45.7% edgema inhibition vs. control when 100mg/kg of dosage was administered, whereas phenylbutazone, 51.4% for 50mg/kg.

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