https://onlinelibrary.wiley.com/doi/pdfdirect/10.1002/ejoc.202101513

Manufacturing Approaches of New Halogenated Agrochemicals

Pre-emergence herbicides are taken up by seeds before germination and by roots, hypocotyls, cotyledons, coleoptiles or leaves before emergence, whereas post-emergence herbicides are taken up primarily by foliage and stems. Most modern pre-emergence herbicides are lipophilic, but post-emergence herbicides may be lipophilic or hydrophilic. The metabolic conversion of herbicides to inactive or active metabolites after plant uptake is of major importance for some compound classes. Several herbicides are proherbicides as for example some acetyl-coenzyme A carboxylase (ACCase)-inhibitors. The physicochemical characteristics of proherbicides and herbicides are usually unrelated. A major role can be attributed to the site of action at a cellular level. A great number of herbicides such as photosystem II (PS II)-inhibitors, protoporphyrinogen oxidase (PPO)-inhibitors or carotenoid biosynthesis inhibitors require light for activity. Others, such as cellulose-biosynthesis and mitotic inhibitors seem to be primarily active in belowground organs. Several lipophilic barriers against the uptake of xenobiotics exist in aboveground and belowground plant parts. The relevance of these barriers needs, however, further clarification. Uptake and translocation models are valuable tools for the explanation of the potential movement of compounds. Many factors other than uptake and translocation have, however, to be considered for the design of herbicides. For post-emergence herbicides, ultraviolet (UV) light stability, stability in formulations, and mixability with other agrochemicals have to be kept in mind while, in addition to the aforementioned factors soil interaction plays a major role for pre-emergence herbicides. In our opinion, general physicochemical characteristics of pre- or post-emergence herbicides do, unfortunately not exist yet. © 2021 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

What makes a molecule a pre- or a post-herbicide - how valuable are physicochemical parameters for their design?

To ensure ongoing sustainability, the modern agrochemical industry is faced with enormous challenges. These arise from provision of high-quality food to increasing water use and environmental impact as well as growing world population. The loss of previous agrochemicals due to consumer perception, changing grower needs and everchanging regulatory requirements is higher than the number of active ingredients can being introduced into the crop protection market. Therefore, the development of novel agrochemicals is essential, that can provide improved efficacy and environmental profiles. In this context, introduction of fluorine atoms and fluorine-containing motifs into a molecule is an important method to influence its physicochemical properties. These include for example small difluoro- and trifluoromethyl, or trifluoromethoxy groups at aryl or heterocyclic aryl moieties but also fragments like 2,2,2-trifluoroethoxycarbonyl, trifluoromethylsulfonyl, trifluoroacetyl, as well as the so far unusal rest like heptafluoro-iso-propyl. This review gives an overview of recent developments of fluorine-containing pesticides launched over the past 7 years and describes a selection of current fluorine-containing development candidates. This article is protected by copyright. All rights reserved.

Recent developments in fluorine-containing pesticides.

For a long time, fungal pathogens have been a threat to the health and diet of humans. Consequently, antimycotic agents have been developed, which are called fungicides in agriculture and antifungals in medicine. Because fungi constantly develop resistance to established modes of action and because of the need for reducing the required use rates/doses, immense research efforts are still being undertaken to discover novel antimycotics. The research-based agrochemical industry has proven that these requirements can be fulfilled by a constant flow of novel fungicidal modes of action, the expansion of agronomical scope and applicability of existing fungicidal mode of action classes, and the design of resistance-breaking active ingredients in an established fungicidal mode of action class, if the molecular structure of the mutated fungal strain is known. Such strategies could be also useful for the discovery of novel antifungals.

Latest Research Trends in Agrochemical Fungicides: Any Learnings for Pharmaceutical Antifungals?

Design, synthesis, and fungicidal evaluation of novel oxysterol binding protein inhibitors for combatting resistance associated with oxathiapiprolin.

Accumulation of very long chain fatty acids (VLCFAs) due to defects in ATP binding cassette protein D1 (ABCD1) is thought to underlie the pathologies observed in adrenoleukodystrophy (ALD). Pursuing a substrate reduction approach based on the inhibition of elongation of very long chain fatty acid 1 enzyme (ELOVL1), we explored a series of thiazole amides that evolved into compound 27─a highly potent, central nervous system (CNS)-penetrant compound with favorable in vivo pharmacokinetics. Compound 27 selectively inhibits ELOVL1, reducing C26:0 VLCFA synthesis in ALD patient fibroblasts, lymphocytes, and microglia. In mouse models of ALD, compound 27 treatment reduced C26:0 VLCFA concentrations to near-wild-type levels in blood and up to 65% in the brain, a disease-relevant tissue. Preclinical safety findings in the skin, eye, and CNS precluded progression; the origin and relevance of these findings require further study. ELOVL1 inhibition is an effective approach for normalizing VLCFAs in models of ALD.

Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.

Oxysterol‐binding Protein Inhibitors: Oxathiapiprolin – A New Oomycete Fungicide That Targets An Oxysterol‐binding Protein

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Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.

Oxysterol‐binding Protein Inhibitors: Oxathiapiprolin – A New Oomycete Fungicide That Targets An Oxysterol‐binding Protein