title: Discovery of Rigidified α,β-Unsaturated Imines as New Resistance-breaking Insecticides for Malaria Vector Control.
abstract: 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.
authors: Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany.
authors: Alexander
authors: A
authors: Arlt
authors: Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany.
authors: Niels
authors: N
authors: Böhnke
authors: Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany.
authors: Sebastian
authors: S
authors: Horstmann
authors: Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany.
authors: Arnoldus W P
authors: AW
authors: Vermeer
authors: Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany.
authors: Stefan
authors: S
authors: Werner
authors: Bayer CropScience AG Pest Control Chemistry Alfred-Nobel-Str. 50 D-40789 Monheim, Germany. robert.velten@bayer.com.
authors: Robert
authors: R
authors: Velten
mesh_terms: D000818:Animals; D055808:Drug Discovery; D007097:Imines / Q000494:pharmacology*; D007303:Insect Vectors; D007305:Insecticide Resistance; D007306:Insecticides / Q000138:chemical synthesis / Q000494:pharmacology*; D008288:Malaria / Q000517:prevention & control*; D009032:Mosquito Control / Q000379:methods*
chemical_list: D007097:Imines; D007306:Insecticides