Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 3 de 3
Filter
Add more filters










Database
Language
Publication year range
1.
Bioorg Med Chem Lett ; 27(4): 911-917, 2017 Feb 15.
Article in English | MEDLINE | ID: mdl-28087271

ABSTRACT

A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species. In this communication, we report the part of the optimization program that led to the identification of dicloromezotiaz as a potent insecticide to control a broad range of lepidoptera. Our efforts in discovery, synthesis, structure-activity relationship elucidation, and biological activity evaluation are also presented.


Subject(s)
Lepidoptera/drug effects , Pyrimidinones/chemistry , Pyrimidinones/pharmacology , Receptors, Nicotinic/metabolism , Animals , Insecticides/chemistry , Insecticides/pharmacology , Protein Binding/drug effects , Receptors, Nicotinic/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett ; 27(1): 16-20, 2017 Jan 01.
Article in English | MEDLINE | ID: mdl-27894871

ABSTRACT

A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species. In this communication, we report the part of the optimization program which led to the discovery of triflumezopyrim as a highly potent insecticide controlling various hopper species. Our efforts in discovery, synthesis, structure-activity relationship elucidation, and biological activity evaluation are also presented.


Subject(s)
Drug Discovery , Insecticides/pharmacology , Orthoptera/drug effects , Pyridines/pharmacology , Pyrimidinones/pharmacology , Animals , Dose-Response Relationship, Drug , Insecticides/chemistry , Molecular Structure , Pyridines/chemistry , Pyrimidinones/chemistry , Species Specificity , Structure-Activity Relationship
3.
Bioorg Med Chem ; 24(3): 354-61, 2016 Feb 01.
Article in English | MEDLINE | ID: mdl-26314923

ABSTRACT

Oxathiapiprolin is the first member of a new class of piperidinyl thiazole isoxazoline fungicides with exceptional activity against plant diseases caused by oomycete pathogens. It acts via inhibition of a novel fungal target-an oxysterol binding protein-resulting in excellent preventative, curative and residual efficacy against key diseases of grapes, potatoes and vegetables. Oxathiapiprolin is being developed globally as DuPont™ Zorvec™ disease control with first registration and sales anticipated in 2015. The discovery, synthesis, optimization and biological efficacy are presented.


Subject(s)
Drug Discovery , Hydrocarbons, Fluorinated/pharmacology , Oomycetes/drug effects , Oomycetes/metabolism , Pyrazoles/pharmacology , Receptors, Steroid/antagonists & inhibitors , Dose-Response Relationship, Drug , Hydrocarbons, Fluorinated/chemical synthesis , Hydrocarbons, Fluorinated/chemistry , Molecular Structure , Pyrazoles/chemical synthesis , Pyrazoles/chemistry , Structure-Activity Relationship
SELECTION OF CITATIONS
SEARCH DETAIL
...