Synthesis and fungicidal activity of 1,1-diaryl tertiary alcohols.

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. Copyright © 2016. Published by Elsevier Ltd.

Citation

Xiuyun Li, Xiaoqiang Han, Mengmeng He, Yumei Xiao, Zhaohai Qin. Synthesis and fungicidal activity of 1,1-diaryl tertiary alcohols. Bioorganic & medicinal chemistry letters. 2016 Dec 15;26(24):5936-5942

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PMID: 27838182

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