16 research outputs found

    Access to “Friedel–Crafts-Restricted” <i>tert</i>-Alkyl Aromatics by Activation/Methylation of Tertiary Benzylic Alcohols

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    Herein we describe a two-step protocol to prepare <i>m</i>-<i>tert</i>-alkylbenzenes. The appropriate tertiary benzylic alcohols are activated with SOCl<sub>2</sub> or concentrated HCl and then treated with trimethylaluminum, affording the desired products in 68–97% yields (22 examples). This reaction sequence is successful in the presence of a variety of functional groups, including acid-sensitive and Lewis-basic groups. In addition to <i>t</i>-Bu groups, 1,1-dimethylpropyl and 1-ethyl-1-methylpropyl groups can also be installed using this method

    Understanding cultivar-specificity and soil determinants of the cannabis microbiome.

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    Understanding microbial partnerships with the medicinally and economically important crop Cannabis has the potential to affect agricultural practice by improving plant fitness and production yield. Furthermore, Cannabis presents an interesting model to explore plant-microbiome interactions as it produces numerous secondary metabolic compounds. Here we present the first description of the endorhiza-, rhizosphere-, and bulk soil-associated microbiome of five distinct Cannabis cultivars. Bacterial communities of the endorhiza showed significant cultivar-specificity. When controlling cultivar and soil type the microbial community structure was significantly different between plant cultivars, soil types, and between the endorhiza, rhizosphere and soil. The influence of soil type, plant cultivar and sample type differentiation on the microbial community structure provides support for a previously published two-tier selection model, whereby community composition across sample types is determined mainly by soil type, while community structure within endorhiza samples is determined mainly by host cultivar

    Mosquito Acetylcholinesterase as a Target for Novel Phenyl-Substituted Carbamates

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    New insecticides are needed for control of disease-vectoring mosquitoes and this research evaluates the activity of new carbamate acetylcholinesterase (AChE) inhibitors. Biochemical and toxicological characterization of carbamates based on the parent structure of terbam, 3-tert-butylphenyl methylcarbamate, was performed. In vitro enzyme inhibition selectivity (Anopheles gambiae versus human) was assessed by the Ellman assay, as well as the lethality to whole insects by the World Health Organization (WHO) paper contact assay. Bromination at the phenyl C6 position increased inhibitory potency to both AChEs, whereas a 6-iodo substituent led to loss of potency, and both halogenations caused a significant reduction of mosquitocidal activity. Similarly, installation of a hexyl substituent at C6 drastically reduced inhibition of AgAChE, but showed a smaller reduction in the inhibition of hAChE. A series of 4-carboxamido analogs of the parent compound gave reduced activity against AgAChE and generally showed more activity against hAChE than AgAChE. Replacement of the 3-t-buyl group with CF3 resulted in poor anticholinesterase activity, but this compound did have measurable mosquitocidal activity. A series of methyl- and fluoro- analogs of 3-trialkylsilyl compounds were also synthesized, but unfortunately resulted in disappointing activity. Finally, a series of sulfenylated proinsecticides showed poor paper contact toxicity, but one of them had topical activity against adult female Anopheles gambiae. Overall, the analogs prepared here contributed to a better understanding of carbamate structure&#8722;activity relationships (SAR), but no new significant leads were generated

    Effects of Microclimate Condition Changes Due to Land Use and Land Cover Changes on the Survivorship of Malaria Vectors in China-Myanmar Border Region

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    <div><p>In the past decade, developing countries have been experiencing rapid land use and land cover changes, including deforestation and cultivation of previously forested land. However, little is known about the impact of deforestation and land-use changes on the life history of malaria vectors and their effects on malaria transmission. This study examined the effects of deforestation and crop cultivation on the adult survivorship of major malaria mosquitoes, <i>Anopheles sinensis</i> and <i>An</i>. <i>minimus</i> in the China-Myanmar border region. We examined three conditions: indoor, forested, and banana plantation. Mean survival time of <i>An</i>. <i>sinensis</i> in banana plantation environment was significantly longer than those in forested environment, and mosquitoes exhibited the longest longevity in the indoor environment. This pattern held for both males and females, and also for <i>An</i>. <i>minimus</i>. To further test the effect of temperature on mosquito survival, we used two study sites with different elevation and ambient temperatures. Significantly higher survivorship of both species was found in sites with lower elevation and higher ambient temperature. Increased vector survival in the deforested area could have an important impact on malaria transmission in Southeast Asia. Understanding how deforestation impacts vector survivorship can help combat malaria transmission.</p></div

    Daily dynamics of microclimatic conditions.

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    <p>Dynamics of hourly indoor temperature (<b>A</b>), relative humidity (<b>B</b>) and light intensity (C) under three land use and land cover conditions.</p
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