Miracles of Synthesis: Fast Acting Insecticides for Vector Control

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Miracles of Synthesis Fast Acting Insecticides
for Vector Control

• Kamlesh Chauhan, Thanh Le, and Ulrich Bernier
• United States Department of Agriculture,
  Agriculture Research Services
• Deployed War Fighter Protection Symposium
• American Mosquito Control Association
• March 5, 2008

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Research Objectives

• Design and investigate fast acting insecticides
• Identify and develop new active chemistries
• to balance vapor pressure and toxicity.
• Formulation of novel insecticides

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Logistics
WRAIR Ed Rowton Maj. Lawrence Apu Bhattacharjee
USUHS John Grieco Nicole Aachee
NMRCD, Peru LCDR. Florin Greg Divine
USAMRU, Kenya Maj. Richardson Col. Gordon
IIBBL Chemistry
CMAVE Uli Bernier Dan Kline Jerry Hogsette
Industrial Partners MGK Badoukien BASF
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Alchemist
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Bioassays
KD Module (in vitro) measures feeding
deterrence and toxicity
HTS Chamber measures contact irritancy spatial
repellency and toxicity
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Feeding deterrence and toxicity
Attraction inhibition
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Bottle-neck assay

• Commercial viability?
• candidate with chiral centers, cost of
  synthesis, degradation products, residual effects
• Toxicity?
• Mode of action?
• Other applications?

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1. Design and investigate fast acting
insecticides
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New Pyrethroids with desired vapor action
62 new compounds have been synthesized 14
actives 5 have been streamlined for patent
application
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Feeding deterrence and toxicity in KD
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3 minutes - too long
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Knockdown (toxicity)
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Duration?

• TL-105,107, 139 and 141 exhibited 100
• mortality up to 48 hours at 25 nM/cm2.
• at 2.5 nM/cm2 TL-105,107, 139 and 141 exhibited
  100 mortality up to 24 hours, at 48 hrs there
  was 8-10 reduction in mortality

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Patent Application

• Invention Disclosure (2006) Identification of
  key ligand in the development of more effective
  deterrents and toxicants of arthropod vectors.
• Invention Disclosure Received 06/05/06
• Approved by Institute 06/20/06
• Docket Number U 0048.06