|Slavov, Svetoslav -|
|Katritzky, Alan -|
Submitted to: Meeting Abstract
Publication Type: Abstract Only
Publication Acceptance Date: March 8, 2010
Publication Date: N/A
Technical Abstract: N,N-diethyl-3-methylbenzamide (DEET) is the most effective and best studied mosquito repellent currently on the market in the U.S.; however, this repellent is not a highly efficacious, repellent of long duration that prevents bites from all medically important mosquito species, especially those that transmit malaria parasites. The current research is driven by the U.S. military’s need for more effective products that will have higher user acceptability rates to prevent bites from malaria vectors, such as Anopheles gambiae and An. albimanus. Current collaborative research between the United States Department of Agriculture (USDA)-Agricultural Research Service and the University of Florida, Department of Chemistry involves state-of-the-art modeling, organic synthesis and laboratory bioassays using human volunteers. Initial repellency data were selected from USDA archives which have been compiled over the last six decades. Two classes of compounds, carboxamides and acylpiperidines, were evaluated against mosquitoes and these data were used to develop Quantitative Structure Activity Relationship (QSAR) models. Of the 64 compounds predicted by the QSAR modeling and tested, more than 20 protected volunteers from mosquito bites longer than DEET. This research demonstrates that QSAR modeling approaches are an effective means of identifying better repellents.