Author
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TABANCA, NURHAYAT - University Of Mississippi |
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KOCYIGIT-KAYMAKCIOGL, BEDIA - Marmara Research Center |
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BEYHAN, NAGIHAN - Marmara Research Center |
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Bernier, Ulrich |
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ALI, ABBAS - University Of Mississippi |
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KHAN, IKHLAS - University Of Mississippi |
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BLOOMQUIST, JEFFREY - University Of Florida |
Submitted to: Meeting Abstract
Publication Type: Abstract Only Publication Acceptance Date: 3/4/2016 Publication Date: N/A Citation: N/A Interpretive Summary: Technical Abstract: Aedes aegypti (L.) (Diptera: Culicidae) transmit pathogens to humans, leading to diseases such as yellow fever and dengue fever. Repellents and insecticides are two common interventions to reduce mosquito biting and thereby disease risk. However, overreliance on a chemical or class of chemicals can lead to the development of insecticide resistance in the target pests. Therefore, there is an urgent need for development of alternative insecticides and repellents to reduce or prevent human-received bites from these important vectors. In this study, 25 compounds comprised of a series of chalcones (1a-i), 2-pyrazoline-1-carbothioamides (2a-i), and 2-pyrazoline-1-carboxamide derivatives (3a-g) were synthesized and screened for biting deterrency, repellency, and larvicidal activities. Biting deterrency against Ae. aegypti was evaluated using an in vitro K&D module system. Compounds (1g, 2a, 2e) had the highest biting deterrency (Biting Deterrence Index (BDI) of 0.85, 0.83 and 0.8, respectively) which was close to that of DEET. BDI values near 1 indicate efficacy similar to that of DEET, while values near 0 indicate deterrency similar to that of a negative control. The compounds were subsequently tested in human-based repellent bioassays in order to find their minimum effective dosage (MED), which is the threshold concentration where a repellent begins to fail. These compounds did not repel Ae. aegypti at 0.375, 0.094 and 0.375 mg/cm2 respectively, compared to DEET (0.004 ± 0.002 mg/cm2). All 25 compounds were also screened as larvicides against 1st instar Ae. aegypti larvae and only 1e, 1f and 2g had larvicidal activity with LC50 values of 2.58 ppm, 5.69 ppm and 15.14 ppm, respectively. Based on our findings, chalcone and 2-pyrazoline-1-carbothioamides are good lead structures for the design of new derivatives to controlling mosquitoes, and potentially, other pests. |