Discovery, synthesis, and evaluation of N-substituted amino-2(5H)-oxazolones as novel insecticides activating nicotinic acetylcholine receptors.
N-Substituted amino-2(5H)-oxazolones A are a novel class of insecticides acting as nicotinic acetylcholine receptor (nAChR) agonists and show potent activity against hemipteran insect species. Here we report the discovery and preparation of this class of chemistry. Our efforts in SAR elucidation, biological activity evaluation, as well as mode-of-action studies are also presented.
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA. Electronic address: wenming.zhang@dupont.com.
Wenming
W
Zhang
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
James D
JD
Barry
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
Daniel
D
Cordova
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
Stephen F
SF
McCann
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
Eric A
EA
Benner
DuPont Crop Protection, Stine-Haskell Research Center, 1090 Elkton Road, Newark, DE 19711, USA.
Kenneth A
KA
Hughes
D000586:Amination; D000818:Animals; D007313:Insecta / Q000187:drug effects* / Q000502:physiology; D007306:Insecticides / Q000737:chemistry* / Q000633:toxicity; D010081:Oxazolone / Q000737:chemistry* / Q000633:toxicity; D011978:Receptors, Nicotinic / Q000378:metabolism
D007306:Insecticides; D011978:Receptors, Nicotinic; D010081:Oxazolone
Acetylcholine receptor; Insecticide; Neonicotinoid; Oxazolone