title: Synthesis and fungicidal activity of 1,1-diaryl tertiary alcohols.
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.
authors.affiliation: Department of Applied Chemistry, China Agricultural University, Beijing 100193, China.
authors.forename: Xiuyun
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Agricultural, Shihezi University, Shihezi 832000, China.
authors.forename: Xiaoqiang
authors.initials: X
authors.lastname: Han
authors.affiliation: Department of Applied Chemistry, China Agricultural University, Beijing 100193, China.
authors.forename: Mengmeng
authors.initials: M
authors.lastname: He
authors.affiliation: Department of Applied Chemistry, China Agricultural University, Beijing 100193, China. Electronic address: xiaoyumei@cau.edu.cn.
authors.forename: Yumei
authors.initials: Y
authors.lastname: Xiao
authors.affiliation: Department of Applied Chemistry, China Agricultural University, Beijing 100193, China. Electronic address: qinzhaohai@263.net.
authors.forename: Zhaohai
authors.initials: Z
authors.lastname: Qin
mesh_terms: D000438:Alcohols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000881:Anthrax / Q000188:drug therapy*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001203:Ascomycota / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005659:Fungicides, Industrial / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010935:Plant Diseases; D013329:Structure-Activity Relationship
chemical_list: D000438:Alcohols; D000935:Antifungal Agents; D005659:Fungicides, Industrial
keywords: 1,1-Diaryltertiary alcohol; Fungicidal activity; Structure-activity relationship (SAR)