Abstract
| - Five fluorine-containing 4,4-dihydroxylmethyl-2-aryliminooxazolidines and five 4,4-dihydroxylmethyl-2-aryliminothiazolidines were synthesized and evaluated for their inhibitory activity againsttrehalase in vitro. All these compounds were very readily synthesized compared with the naturaltrehalase inhibitors. They had moderate inhibitory activity toward trehalase, and showed larvicidalactivity and inhibition action to insect flight. The steric parameters and semiempirical quantumparameters of these compounds were acquired by using the molecular modeling method and thePM3-SCF-MO method, respectively. A quantitative structure−activity relationship between half-inhibitory concentrations toward trehalase and the above parameters was established. Keywords: Fluorine-containing 4,4-dihydroxylmethyl-2-anilinooxazo(thiazo)lidines; trehalaseinhibitors; insect flight; synthesis; QSAR
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