Esters and Carbamates as Insecticidal Juvenile Hormone Mimics

Rendler, Sebastian

doi:10.1002/9783527693931.ch32

Cited by 1 publication

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References 15 publications

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“…Juvenile hormone I ( 88 ) and related analogs play a crucial role in the regulation of molting and metamorphosis processes in insects. Application of synthetic juvenile hormone analogs, such as methoprene ( 89 ), which adopts a huge portion of 88 's scaffold, prevents the formation of adult insect stages . Although dioxapyrrolomycin ( 90 ), isolated from the fermentation broth of Streptomyces fumanus , had broad but moderate insecticidal and acaricidal activity as an uncoupler of oxidative phosphorylation, its relatively high oral mammalian toxicity precluded it from being developed.…”

Section: Scaffold Hopping From Naturementioning

confidence: 99%

Agrochemical lead optimization by scaffold hopping

Lamberth

2017

Pest Management Science

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Scaffold hopping, the exchange of a specific portion of a potential active ingredient with another substructure with the aim of finding isofunctional molecular structures with significantly different molecular backbones, often offers the chance in lead discovery or optimization to mitigate problems related to toxicity, intellectual property, and insufficient potency or stability. Scaffold hopping tools such as isosteric ring replacement including 1,3 nitrogen shift and cyclic imine-amide isosterism, but also ring opening and ring closure approaches, functional group isosterism, reversion of functional groups, chain shortening, chain lengthening, and scaffolds delivered by natural products, have become a permanent fixture of the innovation and optimization process in crop protection research. Their appropriate use will be explained through examples of success stories in the field of agrochemistry. Analogies to, but also differences from, the main categories of scaffold hopping in medicinal drug discovery are discussed. © 2017 Society of Chemical Industry.

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Section: Scaffold Hopping From Naturementioning

confidence: 99%

Agrochemical lead optimization by scaffold hopping

Lamberth

2017

Pest Management Science

View full text Add to dashboard Cite

show abstract

Esters and Carbamates as Insecticidal Juvenile Hormone Mimics

Cited by 1 publication

References 15 publications

Agrochemical lead optimization by scaffold hopping

Agrochemical lead optimization by scaffold hopping

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