SummaryMxra8 is a receptor for multiple arthritogenic alphaviruses that cause debilitating acute and chronic musculoskeletal disease in humans. Herein, we present a 2.2 Å resolution X-ray crystal structure of Mxra8 and 4 to 5 Å resolution cryo-electron microscopy reconstructions of Mxra8 bound t...

Trifloxystrobin, fenhexamid and famoxadone belong to the generation of fungicides acting against a broad spectrum of fungi and widely used in Integrated Pest Management strategies in different agricultural crops but mainly in viticulture. In the present work, a gas chromatographic (GC) method fo...

Cyazofamid, famoxadone, mandipropamid and valifenalate, four new fungicides for controlling downy mildew in vine, were applied to an experimental vineyard producing Vitis vinifera white grapes of the Godello variety. Following harvest, the grapes were subjected to single vinification runs. The o...

The response of a commercial strain of Agaricus bisporus (L) Sing to the fungicides famoxadone, tebuconazole and trifloxystrobin was studied in vitro and in vivo. Mycelial growth of A. bisporus on casing medium in tubes was not affected by the reference fungicides carbendazim, prochloraz and man...

The selective fungitoxicity of famoxadone, tebuconazole and trifloxystrobin between a pathogenic strain of Verticillium fungicola (Preuss) Hassebr and Agaricus bisporus (L) Sing was studied in vitro and in mushroom growing rooms. None of the above fungicides was found to be as selective as proch...

Famoxadone (DPX-JE874, Famoxate®) is a highly active, broad-spectrum fungicide from a new class of chemicals, the oxazolidinediones. Famoxadone inhibited sporangial differentiation and zoospore release and caused lysis of zoospores within minutes. Doses in the order of 0.01 mg l−1 were sufficien...

Cymoxanil and famoxadone, the components of Tanos 50DF® (25% a.i. of each product, E.I. du Pont de Nemours and Company, Wilmington, DE) were evaluated alone, together, and in combination with copper hydroxide and/or mancozeb for the control of bacterial spot on tomato and pepper, and bacterial l...

A method was validated for the simultaneous analysis of the residues of dimethomorph, famoxadone and cymoxanil in grape and raisin matrix by ethyl acetate based extraction and liquid chromatography tandem mass spectrometric analysis. Field studies were conducted to evaluate the dissipation rate ...

The residue levels and dissipation rate of famoxadone in watermelon and soil were determined by HPLC-UVD. The LODs for famoxadone in watermelon, peel, flesh and soil were 0.002 mg/kg (0.004 mg/kg in leaf). The fortified recoveries ranged from 84.91% to 99.41% with relative standard deviations (R...

We analyzed the uptake and distribution of two pesticides (famoxadone and oxathiapiprolin) in herbaceous vegetables (cucumber and tomato) and leafy vegetables (Chinese cabbage and lettuce) to test the viability of applying existing archetypes in the dynamic plant uptake model dynamiCROP to model...

The dissipation of famoxadone as well as the behaviour of its metabolites in environmental samples such as water and soil is a major concern. In this study, the dissipation of the target compound in both matrices was carried out applying an analytical method based on ultra-high performance liqui...

Androstenedione analogs containing 7α-substituents have proven to be potent inhibitors of aromatase both in vitro and in vivo. Several of these agents have exhibited higher affinity for the enzyme complex than the substrate. In order to examine further the interaction(s) of 7-substituted steroi...

7-Phenyl-1,4,6-androstatriene-3,17-dione (4), 7-benzyl-1,4,6-androstatriene-3,17-dione (5) and 7-phenethyl-1,4,6-androstatriene-3,17-dione (6) were synthesized and evaluated in vitro in human placental microsomes as enzyme-activated irreversible inhibitors of aromatase. The compounds were synthe...

A series of 7-alkoxyquinolines was synthesized and tested as substrates with hepatic microsomes prepared from male Wistar rats. Microsomal O-dealkylation rates and kinetic constants were determined for the 7-alkoxyquinolines with microsomes from control, 3-methylcholanthrene (MC)-pretreated, and...

N-type calcium channel blockade is a promising therapeutic approach for the treatment of neuropathic pain. Starting from lead compound (S)-1, we focused our optimization efforts on potency for N-type calcium channel inhibition and improvement of CYP inhibition profile. 2-{[(1-Hydroxycyclohexyl)m...

IntroductionSigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 receptor, and synthesized radiobrominated (+)-pBrV. This radiobrominated (+)-pBrV showe...

Chemo- and regioselective addition of anabasine to 3-(1-hydroxycyclohexyl)-2-propynenitrile in ethanol results in 52% yield of a monoadduct, (Z)-3-(1-hydroxycyclohexyl)-3-[2-(3-pyridinyl)piperidino]-2-propenenitrile: in this case, only the piperidine ring of anabasine takes part in the reaction....

In this study, 3β-acetoxy-17β-(1-acetyl-5-(3-pyridinyl)-3-pyrazolinyl) androat-5-ene (AAPP) was synthesized from the reaction of 21(E)-3β–acetoxy–21-(3-pyridinylidene)pregn-5-en-20-one with hydrazine hydrate in acetic acid. The structure of the compound was confirmed by UV–vis, FT-IR, 1H N...

Diverse 2-pyridinyl quinolines 6–12 and 2-pyridinilvinyl quinolines 13–17 were prepared using a straightforward synthesis based on the BiCl3-catalyzed multicomponent imino Diels–Alder (imino DA) reaction or a novel tandem imino DA/catalytic tetrahydroquinoline ring oxidation/Perkin condensati...

ortho-Amidation of 2-pyridinyl ferrocenes with 1,4,2-dioxazol-5-ones was achieved via Cp∗Co(III)-catalyzed direct C-H bond functionalization reaction. In the presence of Cp*Co(CO)I2, in combination with AgPF6 and AgOPiv, a wide range of ferrocene-based amidated products were obtained in up to 96...