RESUMO
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.
Assuntos
Descoberta de Drogas , Inseticidas/farmacologia , Ortópteros/efeitos dos fármacos , Piridinas/farmacologia , Pirimidinonas/farmacologia , Animais , Relação Dose-Resposta a Droga , Inseticidas/química , Estrutura Molecular , Piridinas/química , Pirimidinonas/química , Especificidade da Espécie , Relação Estrutura-AtividadeRESUMO
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.
Assuntos
Lepidópteros/efeitos dos fármacos , Pirimidinonas/química , Pirimidinonas/farmacologia , Receptores Nicotínicos/metabolismo , Animais , Inseticidas/química , Inseticidas/farmacologia , Ligação Proteica/efeitos dos fármacos , Receptores Nicotínicos/química , Relação Estrutura-AtividadeRESUMO
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.