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Article Abstract
A series of 3-aryl propionic esters and their analogues were designed and evaluated for acaricidal activity in vitro against Psoroptes cuniculi, a mange mite. The structure-activity relationship (SAR) was also discussed. The results showed that 6 compounds possessed the excellent activity (LC = 0.17-0.24 mM, LT = 1.5-2.9 h), superior to ivermectin (LC = 0.28 mM, LT = 8.9 h) (P < 0.05), a standard drug. Furthermore, 7 compounds showed the good activity (LC = 0.25-0.37 mM, LT < 3.9 h), slightly lower or close to that of ivermectin. One compound displayed super-fast acaricidal property, far superior to ivermectin. SAR analysis found that the ester group is vital for the activity and the small steric hindrance adjacent to the ester group is advantageous for the high activity. The
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5788918 PMC http://dx.doi.org/10.1038/s41598-018-20140-7 DOI Listing Publication Analysis
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