2013Fine Chemical IntermediatesRequires access

Synthesis and Antifungal Activity of N-(1,4-Substitued-pyrazole-5-yl) 1,2,3-thiadiazole Carboxamide Derivatives

WU Zhi-bin

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Abstract

A series of N-(1,4 disubstituted pyrazole-yl)-1,2,3-thiadiazole carboxamide derivatives were synthesized. All target compounds were bioassayed in vitro against three kinds of phytopathogenic fungi(Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results indicated that most of the synthesized compounds possessed antifungal activities to a certain extent, among which compound 8d displayed 56.8% inhibition against C. mandshurica at 50 μg / mL, and compound 8j displayed 47.6% inhibition against G. zeae at 50 μg / mL. The structures of the target compounds could be further optimized based on the designed compounds.

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What this paper is about

A series of N-(1,4 disubstituted pyrazole-yl)-1,2,3-thiadiazole carboxamide derivatives were synthesized. All target compounds were bioassayed in vitro against three kinds of phytopathogenic fungi(Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results indicated that most of the synthesized compounds possessed antifungal activities to a certain extent, among which compound 8d displayed 56.8% inhibition against C. mandshurica at 50 μg / mL, and compound 8j displayed 47.6% inhibition against G. zeae at 50 μg / mL. The structures of the target compounds could be further optimized based on the designed compounds.

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Available abstract

A series of N-(1,4 disubstituted pyrazole-yl)-1,2,3-thiadiazole carboxamide derivatives were synthesized. All target compounds were bioassayed in vitro against three kinds of phytopathogenic fungi(Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results indicated that most of the synthesized compounds possessed antifungal activities to a certain extent, among which compound 8d displayed 56.8% inhibition against C. mandshurica at 50 μg / mL, and compound 8j displayed 47.6% inhibition against G. zeae at 50 μg / mL. The structures of the target compounds could be further optimized based on the designed compounds.

Key concepts: Gibberella zeae, Chemistry, Fusarium oxysporum, Carboxamide, Antifungal, Pyrazole, Stereochemistry, In vitro

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Synthesis and Antifungal Activity of N-(1,4-Substitued-pyrazole-5-yl) 1,2,3-thiadiazole Carboxamide Derivatives — Research Paper | ScholarLens