Discovery of Rigidified ?,?-Unsaturated Imines as New Resistance-breaking Insecticides for Malaria Vector Control

Authors

  • Alexander Arlt Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany
  • Niels Böhnke Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany
  • Sebastian Horstmann Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany
  • Arnoldus W. P. Vermeer Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany
  • Stefan Werner Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany
  • Robert Velten Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany. robert.velten@bayer.com

DOI:

https://doi.org/10.2533/chimia.2016.694

Keywords:

Anopheles, Conformational rigidification, Malaria, α,β-unsaturated imines, Vinyl sulphides

Abstract

During our continuous search for new resistance-breaking insecticides applicable to malaria vector control, a new class of ?,?-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.

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Published

2016-10-26

Issue

Section

Scientific Articles

How to Cite

[1]
A. Arlt, N. Böhnke, S. Horstmann, A. W. P. Vermeer, S. Werner, R. Velten, Chimia 2016, 70, 694, DOI: 10.2533/chimia.2016.694.