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United States Department of Agriculture

Agricultural Research Service

Title: Modeling, Synthesis and Bioassay of Acylpiperidines and Carboxamides As Improved Mosquito Repellents

item Tsikolia, Maia
item Bernier, Ulrich
item Slavov, Svetoslav -
item Agramonte, Natasha
item Clark, Gary
item Linthicum, Kenneth
item Katritzky, Alan -

Submitted to: Meeting Abstract
Publication Type: Abstract Only
Publication Acceptance Date: July 11, 2010
Publication Date: N/A

Technical Abstract: Novel mosquito repellents are being designed through collaborative research between the United States Department of Agriculture (USDA)-Agricultural Research Service and the University of Florida, Department of Chemistry. The approach involves state-of-the-art modeling, organic synthesis, and repellency screening in laboratory bioassays with Aedes aegypti mosquitoes. Quantitative Structure Activity Relationship (QSAR) models are developed based on historical data from the USDA archives for two selected compound classes, carboxamides and acylpiperidines. On the basis of the predictions, 64 compounds were selected and synthesized for repellency screening. The screening process involves testing cloth treated at a known concentration of candidate repellent. The treated cloth is affixed over a rectangular 4 x 8 cm opening cut in a vinyl sleeve that is worn over a layer of nylon stocking on the forearm of a human volunteer. One third of the evaluated compounds protected volunteers from mosquito bites for a longer duration than the standard repellent N,N-diethyl-3-methylbenzamide (deet). This research demonstrates that a combinatorial approach: modeling, synthesis and bioassay is a promising way to design better repellents.

Last Modified: 4/22/2015
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