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  • Title: Synthesis and fungicidal activity of 1,1-diaryl tertiary alcohols.
    Author: Li X, Han X, He M, Xiao Y, Qin Z.
    Journal: Bioorg Med Chem Lett; 2016 Dec 15; 26(24):5936-5942. PubMed ID: 27838182.
    Abstract:
    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.
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