2-噻唑酰氨基环己烷基磺酰胺的合成与杀菌活性

为进一步研究环烷基磺酰胺类化合物的杀菌活性与构效关系，在前期工作基础上，合成了11个未见文献报道的2-噻唑酰氨基环己烷基磺酰胺类化合物 ( 7a ~ 7k )，其结构均经1H NMR、13C NMR、质谱和元素分析确证。分别采用菌丝生长速率法、黄瓜活体叶片法、孢子萌发法和番茄活体盆栽法对目标化合物进行了生物活性测定。结果表明:目标化合物对番茄灰霉病菌Botrytis cinerea表现出较好的抑制活性，其中化合物 7a 和 7c 在10 mg/L下对番茄灰霉病菌孢子萌发的抑制率分别为90%和67%；在200 mg/L 施药剂量下，对活体黄瓜叶片、番茄叶片和番茄花上灰霉病的防治效果，化合物 7a 分别为75%、78%和30%，化合物 7c 分别为78%、62%和44%，均优于对照药剂腐霉利，有进一步研究的价值。

Synthesis and fungicidal activity evaluation of 2-thiazolyl amide cyclohexane-sulfonamide

In order to further explore the fungicidal activities and structure-activity relationship of cycloalkylsulfonamides, based on previous work, 11 novel 2-thiazolylamino cyclohexanesulfonamides were synthesized. Their structures were characterized by ¹H NMR, ¹³C NMR, MS and elemental analysis. The bioactivities of the target compounds was determined by adopting mycelium growth rate method, in vivo cucumber leaves method, spore germination method and in vivo tomato potted method. The bioassay exhibited that the target compounds showed good inhibitory activities against Botrytis cinerea. Among them, the inhibitory rates of compounds 7a and 7c against spore germination of B. cinerea at 10 mg/L were respectively 90% and 67%. With the application dose of 200 mg/L, the control efficacy of compound 7a against gray mold on live cucumber leaves, tomato leaves and tomato flowers were respectively 75%, 78% and 30% and the corresponding control effects of compound 7c were respectively 78%, 62%, and 44%, which were better than procymidone and worth further research.