Bioorganic & medicinal chemistry letters · 2016
Synthesis and fungicidal activity of 1,1-diaryl tertiary alcohols.
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Li Xiuyun, Han Xiaoqiang, He Mengmeng, Xiao Yumei, Qin Zhaohai
Аннотация
A series of 1,1-diaryl tertiary alcohols and some of their dehydration derivatives were designed, synthesized and evaluated for their antifungal activities. Some compounds exhibited moderate inhibitory activities against seven plant pathogens at 50μg/mL in vitro, compounds 5g and 7c displayed nearly the same or higher fungicidal activities against some certain plant pathogens compared with the lead compound pyrimorph. A qualitative structure-activity relationship (SAR) analysis revealed that the Cl substituent and its position at the pyridine ring were crucial for the compounds' activities. Specially, several compounds displayed 100% protection effect against wheat powdery mildew or cucumber anthrax at 400mg/mL in vivo, which suggested that these compounds might be potential fungicidal candidates for certain plant diseases.