Twenty-one novel pyrazole-thiazole carboxamide derivatives were rationally designed and synthesized. Bioassay results indicated that 6d (EC = 5.11 μg/mL) and 6j (EC = 8.14 μg/mL) exhibited better in vitro activities than fluxapyroxad (EC = 11.93 μg/mL) and thifluzamide (EC = 22.12 μg/mL) against Rhizoctonia cerealis. Particularly, compound 6j showed promising in vivo protective activity against Rhizoctonia solani and Puccinia sorghi Schw. with 80% and 90% inhibition at 10 μg/mL, respectively. Our studies found that pyrazole-thiazole is a promising fungicide lead deserving for further derivation.
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Design, synthesis and fungicidal activity of pyrazole-thiazole carboxamide derivatives.
Mol Divers
February 2022
State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, No. 94, Weijin Road, Nankai District, Tianjin, 300071, People's Republic of China.
Twenty-one novel pyrazole-thiazole carboxamide derivatives were rationally designed and synthesized. Bioassay results indicated that 6d (EC = 5.11 μg/mL) and 6j (EC = 8.
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State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, P. R. China.
Succinate dehydrogenase (SDH) is regarded as a promising target for fungicide discovery. To continue our ongoing studies on the discovery of novel SDH inhibitors as fungicides, novel pyrazole-thiazole carboxamides were designed, synthesized, and evaluated for their antifungal activity. The results indicated that compounds , , and showed excellent activities against with EC values from 1.
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Genetic Engineering and Biotechnology Research Institute (GEBRI), Mubarak City for Scientific Research and Technology Application, Borg El-Arab, Alexandria, Egypt.
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