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Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Novel Pyrazole-4-carboxamide Derivatives with a Tetrahydroquinoline Skeleton: Promising SDHIs for the Control of
Bo Luo1,2, Yanbing Wu1,2, Qingsi Zhang3
1Henan Key Laboratory of Tea Plant Biology, Xinyang Key Laboratory of Food Innovation for Tea and Camellia Oleifera, College of Tea and Food Science, Xinyang Normal University, Xinyang464000, Henan, China.
Abstract:
In this study, 30 tetrahydroquinoline-based pyrazole-4-carboxamide derivatives were designed, synthesized, and screened for antifungal activities. Among them, compound 6m displayed the strongest inhibitory activity against Rhizoctonia solani, with a half-maximal effective concentration (EC50) as low as 0.03 μg/mL, superior to Boscalid (EC50 = 0.40 μg/mL) and Fluxapyroxad (EC50 = 0.06 μg/mL). Further detached-leaf assays on rice verified that 6m could markedly suppress the growth of R. solani with strong protective and curative effects even at 50 μg/mL. Follow-up mechanistic studies indicated that compound 6m might exert antifungal activity through SDH inhibition-related mechanisms. These findings suggested that compound 6m might be a potent candidate as a succinate dehydrogenase inhibitor (SDHI) against R. solani. Further research, including field trials and biosafety assessment, was needed to realize the potential of compound 6m as an effective tool for rice protection.
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