Location: Mosquito and Fly ResearchTitle: Synthesis and mosquitocidal activity of a series of hydrazone derivatives against Aedes aegypti
|Altintop, Mehlika - Anadolu Universtiy|
|Bloomquist, Jeffrey - University Of Florida|
|Kaplancikli, Zafer - Anadolu Universtiy|
|Özdemir, Ahmet - Anadolu Universtiy|
Submitted to: Letters in Drug Design & Discovery
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 9/7/2017
Publication Date: 6/1/2018
Citation: Altintop, M.D., Tabanca, N., Becnel, J.J., Bloomquist, J.J., Kaplancikli, Z.A., Özdemir, A. 2018. Synthesis and mosquitocidal activity of a series of hydrazone derivatives against Aedes aegypti. Letters in Drug Design & Discovery. https://doi.org/10.2174/1570180814666171002155548.
Interpretive Summary: Hydrazones constitute an important class of lead compounds for new drug discovery including new insecticides. Mosquitoes have become highly resistant to the most commonly used pesticides and there is a pressing need for compounds with alternative modes of action. Structural modification of hydrazones produced a series of 16 new compounds that were screened against Aedes aegypti mosquito larvae and adults to determine mosquitocidal activity. Two compounds showed good larvicial activity against mosquitoes and represent new lead compounds for further evaluation.
Technical Abstract: Background: Aedes aegypti is an important mosquito vector for the transmission of several infectious diseases. Current insecticides play a vital role in controlling mosquitoes; however, the frequent use of insecticides has led to the development of insecticide resistance. In order to control mosquito populations, new and effective bioactive molecules are urgently needed. Methods: In the current work, N-(benzylidene)-3-cyclopentylpropionic acid hydrazide derivatives (1-16) were synthesized and evaluated for their larvicidal and adulticidal effects on Ae. aegypti. Results: N-(Benzylidene)-3-cyclopentylpropionic acid hydrazide (1) and N-(4-isopropylbenzylidene)-3-cyclopentylpropionic acid hydrazide (9) displayed good larvicidal activity with LC50 values of 0.010 (0.005-0.017, 95%CI) µg/µL and 0.273 (0.223-0.336, 95%CI) µg/µL, respectively against 1st instar Ae. aegypti. On the other hand, compounds 1-16 showed weak adulticial activity against adult female Ae. aegypti. Conclusion: Due to their notable larvicidal activity, compounds 1 and 9 stand out as promising candidates for further studies.