Discovery of Rigidified α,β-Unsaturated Imines as New Resistance-breaking Insecticides for Malaria Vector Control
During our continuous search for new resistance-breaking insecticides applicable to malaria vector control, a new class of α,β-unsaturated imines was identified by applying the principle of conformational rigidification as a powerful tool for compound optimisation. Herein we describe the successful...
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| Veröffentlicht in: | Chimia 2016-10, Vol.70 (10), p.694-697 |
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| container_title | Chimia |
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| creator | Arlt, Alexander Böhnke, Niels Horstmann, Sebastian Vermeer, Arnoldus W P Werner, Stefan Velten, Robert |
| description | During our continuous search for new resistance-breaking insecticides applicable to malaria vector control, a new class of α,β-unsaturated imines was identified by applying the principle of conformational rigidification as a powerful tool for compound optimisation. Herein we describe the successful synthesis of these compounds and their biological test results. Our lead compound 16 from this insecticidal class outperforms market standards, notably for the control of mosquito strains that exhibit either metabolic or target-site resistance to these established insecticides. In our model system for insecticide-treated mosquito nets the compound reveals long-lasting efficacy for up to several months. |
| doi_str_mv | 10.2533/chimia.2016.694 |
| format | Article |
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| ispartof | Chimia, 2016-10, Vol.70 (10), p.694-697 |
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| language | eng |
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| source | MEDLINE; DOAJ Directory of Open Access Journals |
| subjects | Animals Drug Discovery Imines - pharmacology Insect Vectors Insecticide Resistance Insecticides - chemical synthesis Insecticides - pharmacology Malaria - prevention & control Mosquito Control - methods |
| title | Discovery of Rigidified α,β-Unsaturated Imines as New Resistance-breaking Insecticides for Malaria Vector Control |
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