Design, synthesis and fungicidal activity of pyrazole-thiazole carboxamide derivatives

Twenty-one novel pyrazole-thiazole carboxamide derivatives were rationally designed and synthesized. Bioassay results indicated that 6d (EC50 = 5.11 mu g/mL) and 6j (EC50 = 8.14 mu g/mL) exhibited better in vitro activities than fluxapyroxad (EC50 = 11.93 mu g/mL) and thifluzamide (EC50 = 22.12 mu g/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 mu g/mL, respectively. Our studies found that pyrazole-thiazole is a promising fungicide lead deserving for further derivation. [GRAPHICS] .

Automated summary

Twenty-one novel pyrazole-thiazole carboxamide derivatives were synthesized and evaluated for their fungicidal activities, with compounds 6d and 6j showing promising results both in vitro and in vivo, particularly compound 6j demonstrating good protective activity against Rhizoctonia solani and Puccinia sorghi Schw.