The Unique Role of Fluorine in the Design of Active Ingredients for Modern Crop Protection Export

@article{citeulike:6056482, abstract = {The task of inventing and developing active ingredients with useful biological activities requires a search for novel chemical substructures. This process may trigger the discovery of whole classes of chemicals of potential commercial interest. Similar biological effects can often be achieved by completely different compounds. However, compounds within a given structural family may exhibit quite different biological activities depending on their interactions with different intracellular proteins like enzymes or receptors. By varying the functional groups and structural elements of a lead compound, its interaction with the active site of the target protein, as well as its physicochemical, pharmacokinetic, and dynamic properties can be improved. In this context, the introduction of fluorine into active ingredients has become an important concept in the quest for a modern crop protection product with optimal efficacy, environmental safety, user friendliness, and economic viability. Fluorinated organic compounds represent an important and growing family of commercial agrochemicals. A number of recently developed agrochemical candidates represent novel classes of chemical compounds with new modes of action; several of these compounds contain new fluorinated substituents. However, the complex structure-activity relationships associated with biologically active molecules mean that the introduction of fluorine can lead to either an increase or a decrease in the efficacy of a compound depending on its changed mode of action, physicochemical properties, target interaction, or metabolic susceptibility and transformation. Therefore, it is still difficult to predict the sites in a molecule at which fluorine substitution will result in optimal desired effects.}, address = {Bayer CropScience AG, BCS-R-GCI, Building 6240, Alfred-Nobel-Stra{\ss}e 50, 40789 Monheim am Rhein, Germany, Fax: (+49) 214-30-46410}, author = {Jeschke, Peter}, citeulike-article-id = {6056482}, citeulike-linkout-0 = {http://dx.doi.org/10.1002/cbic.200300833}, citeulike-linkout-1 = {http://www3.interscience.wiley.com/cgi-bin/abstract/108561878/ABSTRACT}, doi = {10.1002/cbic.200300833}, issn = {1439-7633}, journal = {ChemBioChem}, keywords = {agrochemical, fluorination, fluorine, industry}, number = {5}, pages = {570--589}, posted-at = {2009-11-02 14:54:15}, priority = {3}, title = {The Unique Role of Fluorine in the Design of Active Ingredients for Modern Crop Protection}, url = {http://dx.doi.org/10.1002/cbic.200300833}, volume = {5}, year = {2004} }

TY - JOUR ID - citeulike:6056482 L3 - citeulike-article-id:6056482 N2 - The task of inventing and developing active ingredients with useful biological activities requires a search for novel chemical substructures. This process may trigger the discovery of whole classes of chemicals of potential commercial interest. Similar biological effects can often be achieved by completely different compounds. However, compounds within a given structural family may exhibit quite different biological activities depending on their interactions with different intracellular proteins like enzymes or receptors. By varying the functional groups and structural elements of a lead compound, its interaction with the active site of the target protein, as well as its physicochemical, pharmacokinetic, and dynamic properties can be improved. In this context, the introduction of fluorine into active ingredients has become an important concept in the quest for a modern crop protection product with optimal efficacy, environmental safety, user friendliness, and economic viability. Fluorinated organic compounds represent an important and growing family of commercial agrochemicals. A number of recently developed agrochemical candidates represent novel classes of chemical compounds with new modes of action; several of these compounds contain new fluorinated substituents. However, the complex structure-activity relationships associated with biologically active molecules mean that the introduction of fluorine can lead to either an increase or a decrease in the efficacy of a compound depending on its changed mode of action, physicochemical properties, target interaction, or metabolic susceptibility and transformation. Therefore, it is still difficult to predict the sites in a molecule at which fluorine substitution will result in optimal desired effects. IS - 5 JF - ChemBioChem SN - 1439-7633 AD - Bayer CropScience AG, BCS-R-GCI, Building 6240, Alfred-Nobel-Straße 50, 40789 Monheim am Rhein, Germany, Fax: (+49) 214-30-46410 EP - 589 TI - The Unique Role of Fluorine in the Design of Active Ingredients for Modern Crop Protection VL - 5 SP - 570 KW - agrochemical KW - fluorination KW - fluorine KW - industry AU - Jeschke, Peter PY - 2004/// UR - http://dx.doi.org/10.1002/cbic.200300833 ER -