scholarly journals Benzenetriol-Derived Compounds against Citrus Canker

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1436
Author(s):  
Lúcia Bonci Cavalca ◽  
Ciaran W. Lahive ◽  
Fleur Gijsbers ◽  
Fernando Rogério Pavan ◽  
Dirk-Jan Scheffers ◽  
...  
Keyword(s):  
Citrus Canker ◽  
Agricultural Residues ◽  
Copper Salts ◽  
Antibacterial Compounds ◽  
Natural Origin ◽  
Low Toxicity ◽  
Alkyl Ethers ◽  
Citrus Orchards ◽  
Bacterial Cell Membrane ◽  
New Compounds

In order to replace the huge amounts of copper salts used in citrus orchards, alternatives have been sought in the form of organic compounds of natural origin with activity against the causative agent of citrus canker, the phytopathogen Xanthomonas citri subsp. Citri. We synthesized a series of 4-alkoxy-1,2-benzene diols (alkyl-BDOs) using 1,2,4-benzenetriol (BTO) as a starting material through a three-step synthesis route and evaluated their suitability as antibacterial compounds. Our results show that alkyl ethers derived from 1,2,4-benzenetriol have bactericidal activity against X. citri, disrupting the bacterial cell membrane within 15 min. Alkyl-BDOs were also shown to remain active against the bacteria while in solution, and presented low toxicity to (human) MRC-5 cells. Therefore, we have demonstrated that 1,2,4-benzenetriol—a molecule that can be obtained from agricultural residues—is an adequate precursor for the synthesis of new compounds with activity against X. citri.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

STUDY OF ACUTE AND SUBCHRONIC TOXICITY OF DIATOMITE

2021 ◽  
Vol 1 (4) ◽  
pp. 505-513
Author(s):  
Vasiliy I. Dorozhkin ◽  
◽  
Galina I. Pavlenko ◽  
Natalia S. Pavlova ◽  
◽  
...  
Keyword(s):  
Russian Federation ◽  
New Technologies ◽  
Animal Husbandry ◽  
Wound Treatment ◽  
Subchronic Toxicity ◽  
Natural Origin ◽  
White Rats ◽  
Low Toxicity ◽  
The Russian Federation

With the development of new technologies, sorbents of natural origin are becoming more widely used in animal husbandry. One of the promising rocks is diatomite, large reserves of which are available in the Russian Federation. It is promising as an enterosorbent, litter, powder, for wound treatment, etc. The article presents the materials of a study on white rats of acute and subchronic toxicity of diatomite of the Kamyshlovskoye deposit. As a result, data were obtained indicating low toxicity of diatomite under conditions of introduction into the stomach (4th class according to GOST 12.1.007). Diatomite has no material and functional accumulation in the conditions of a subchronic experiment.

scholarly journals Identification of a Novel Antiviral Inhibitor of the Flavivirus Guanylyltransferase Enzyme

2012 ◽  
Vol 86 (16) ◽  
pp. 8730-8739 ◽  
Author(s):  
Hillary J. Stahla-Beek ◽  
Daniel G. April ◽  
Bejan J. Saeedi ◽  
Amanda M. Hannah ◽  
Susan M. Keenan ◽  
...  
Keyword(s):  
Dengue Virus ◽  
High Throughput Screening ◽  
Yellow Fever Virus ◽  
Subgenomic Replicon ◽  
Relationship Analysis ◽  
Gtp Binding ◽  
Capping Enzyme ◽  
Low Toxicity ◽  
Rna Capping ◽  
New Compounds

Arthropod-borne flavivirus infection causes serious morbidity and mortality worldwide, but there are currently no effective antiflaviviral chemotherapeutics available for human use. Therefore, it is critical that new therapeutics against virus-specific targets be developed. To identify new compounds that may be used as broadly active flavivirus therapeutics, we have performed a high-throughput screening of 235,456 commercially available compounds for small-molecule inhibitors of the dengue virus NS5 RNA capping enzyme. We identified a family of compounds, the 2-thioxothiazolidin-4-ones, that show potent biochemical inhibition of capping enzyme GTP binding and guanylyltransferase function. During the course of structure-activity relationship analysis, a molecule within this family, (E)-{3-[5-(4-tert-butylbenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid} (BG-323), was found to possess significant antiviral activity in a dengue virus subgenomic replicon assay. Further testing of BG-323 demonstrated that this molecule is able to reduce the replication of infectious West Nile virus and yellow fever virus in cell culture with low toxicity. The results of this study describe the first inhibitor that targets the GTP-binding/guanylyltransferase activity of the flavivirus RNA capping enzyme.

Synthesis and structure-activity study of quaternary ammonium functionalized β-cyclodextrin-carboxymethylcellulose polymers

2011 ◽  
Vol 63 (12) ◽  
pp. 2827-2832 ◽  
Author(s):  
Danielle Bonenfant ◽  
François-René Bourgeois ◽  
Murielle Mimeault ◽  
Frédéric Monette ◽  
Patrick Niquette ◽  
...  
Keyword(s):  
Quaternary Ammonium ◽  
Antimicrobial Activities ◽  
Bacterial Cells ◽  
Experimental Conditions ◽  
E Coli ◽  
Antimicrobial Efficiency ◽  
Disinfection Process ◽  
Didecyldimethylammonium Chloride ◽  
Low Toxicity ◽  
Bacterial Cell Membrane

Carboxymethylcellulose (CMC) and β-cyclodextrin (β-CD)-based polymers functionalized with two types of quaternary ammonium compounds (QACs), the alkaquat DMB-451 (N-alkyl (50% C14, 40% C12, 10% C10) dimethylbenzylammonium chloride) (DMD-451) named polymer DMB-451, and FMB 1210-8 (a blend of 32 w% N-alkyl (50% C14, 40% C12, 10% C10) dimethylbenzylammonium chloride and 48 w% of didecyldimethylammonium chloride) named polymer FMB 1210-8, were synthethized and characterized by Fourier transform infrared spectroscopy. The antimicrobial activities of these polymers against Eschericia coli were also evaluated at 25 °C in wastewater. The results have indicated that the polymer FMB 1210-8 possesses a high-affinity binding with bacterial cells that induces a rapid disinfection process. Moreover, in the same experimental conditions of disinfection (mixture of 1.0 g of polymer and 100 mL of wastewater), the polymer FMB 1210-8 has a higher antimicrobial efficiency (99.90%) than polymer DMB-451 (92.8%). This phenomenon might be associated to a stronger interaction with bacterial cells due to stronger binding affinity for E. coli cells and greater killing efficiency of the C10 alkyl chains QAC of polymer FMB 1210-8 to disrupt the bacterial cell membrane as compared to N-alkyl (50% C14, 40% C12, 10% C10) dimethylbenzylammonium chloride. Together, these results suggest that the polymer FMB 1210-8 could constitute a good disinfectant against Escherichia coli, which could be advantageously used in wastewater treatments due to the low toxicity of β-CD and CMC, and moderated toxicity of FMB 1210-8 to human and environment.

Darstellung und Charakterisierung substituierter Phosphinoether und -thioether / Preparation and Characterization of Substituted Phosphinoethers and -thioethers

1995 ◽  
Vol 50 (2) ◽  
pp. 168-174 ◽  
Author(s):  
Werner Wolfsberger ◽  
Wolfgang Burkart ◽  
Helmut Werner
Keyword(s):  
Pure State ◽  
Ring Opening ◽  
Nmr Spectra ◽  
Ir And Nmr Spectra ◽  
Elemental Analyses ◽  
Alkyl Ethers ◽  
New Compounds ◽  
Nucleophilic Ring Opening ◽  
Secondary Phosphines

The (diorganophosphinopropyl)alkyl ethers 1-7 are prepared by hydrophosphination of allylalkyl ethers with secondary phosphines. The corresponding thioethers cannot be obtained in a pure state by the same route. The nucleophilic ring opening of thiirane with lithium dialkyl phosphides, followed by the reaction with ClSi(CH3)3 or Cl(CH2)2OCH3 produces the thioethers 8-12 and 16. The silylated thioethers 8, 10 and 12 react with CH3OH/H2O to give the phosphinoethyl thiols 13-15. All new compounds have been identified and characterized by elemental analyses, IR and NMR spectra.

Spray Volume and Rate Based on the Tree Row Volume for a Sustainable Use of Copper in the Control of Citrus Canker

Plant Disease ◽  
2021 ◽  
Vol 105 (1) ◽  
pp. 183-192
Author(s):  
Franklin Behlau ◽  
Fabrício E. Lanza ◽  
Marcelo da Silva Scapin ◽  
Luis Henrique Mariano Scandelai ◽  
Geraldo José Silva Junior
Keyword(s):  
Sweet Orange ◽  
Metallic Copper ◽  
Sustainable Use ◽  
Citrus Canker ◽  
Tree Canopy ◽  
Minimum Threshold ◽  
Diseased Fruit ◽  
Citrus Orchards ◽  
Spray Volume

Copper is the most efficient pesticide for the control of citrus canker (Xanthomonas citri subsp. citri). To mitigate the environmental impacts and costs, the copper sprays in citrus orchards are being optimized based on the tree row volume (TRV). A previous investigation allowed for significant reductions of the spray volume and copper rates. Nevertheless, the results also indicated the need for additional studies. The aim of this work was to assess whether both the spray volume and the metallic copper rate based on the TRV may be further reduced. A field trial was carried out during two seasons in a 3-year-old commercial orchard of Pera sweet orange located in the municipality of Paranavaí, Paraná, Brazil. The volumes of 20 and 40 ml of spray mixture per m3 of the tree canopy were assessed in combination with the metallic copper rates of 10.5, 21.0, 36.8, or 52.5 mg/m3. Disease was measured as the temporal progress of canker incidence on leaves, cumulative dropped fruit with canker, and incidence of diseased fruit at harvest. The quality of sprays was assessed by measuring the copper deposition and leaf coverage. The treatment with the highest citrus canker control for the lowest use of water and copper was the combination of 40 ml and 36.8 mg/m3. Regression analyses indicated that the minimum threshold deposition of copper was ∼1.5 µg Cu2+/cm2 leaf area. In addition, the lowest spray volume and copper rate necessary to achieve this deposition are 35 ml/m3 and 30 mg/m3. The use of 20 ml/m3 did not efficiently control the disease due to the deficient coverage of treated surfaces. This study demonstrated that it is possible to use even lower amounts of copper and water without interfering with the efficiency of control of citrus canker.

The Reactions of Pygosteus Pungitius L. to Toxic Solutions

1947 ◽  
Vol 24 (1-2) ◽  
pp. 110-122
Author(s):  
J. R. ERICHSEN JONES
Keyword(s):  
Tap Water ◽  
Glass Tube ◽  
Negative Reaction ◽  
Small Fish ◽  
Toxic Substances ◽  
Copper Salts ◽  
Concentration Difference ◽  
Low Toxicity ◽  
High Concentrations ◽  
Flowing Solution

An apparatus is described in which small fish (Pygosteus pungitius L.) are confined in a horizontal glass tube, half of which is filled with flowing tap water and half with flowing solution. Solution and water are very sharply differentiated, so that the concentration difference the fish encounter is known. The directions of flow can be rapidly reversed in order to check the result. The movements of the fish are recorded for 7-120 min., according to the degree of toxicity of the substance tested. A negative reaction is shown towards 1% ethyl alcohol, 1/10,000-1/5000 chloroform and 0.1-0.4% formalin (% HCHO). High concentrations of these substances may stupefy the fish so rapidly that a pseudo-positive reaction appears. A sharp negative reaction is displayed towards 0.003-0.001N mercuric chloride; at 0.0003 the reaction is delayed, at 0.0001 is indefinite, and at 0.00004N solution, though of comparatively high toxicity, does not appear to be detected. Zinc sulphate appears to be detected and avoided at concentrations at least as low as 0.0003N. This concentration is of comparatively low toxicity and may be exceeded in streams polluted by effluents from zinc mines. Copper sulphate is only detected and avoided at extremely high concentrations (0.1N). At 0.04N the reaction is vague, and at 0.01-0.001N the fish swim into the solution where they become stupefied and lie motionless, so that the reaction appears positive. Copper salts appear to impair or destroy the stickleback's ability to distinguish other toxic substances.

Synthesis and Antibacterial Activity of some New Quinoxaline-1,4-Dioxide Derivatives

2013 ◽  
Vol 634-638 ◽  
pp. 1376-1379 ◽  
Author(s):  
Zhi Jun Xin ◽  
Jian Ping Liang ◽  
Xue Hu Li ◽  
Lei Tao ◽  
Xi Hong Lu
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Good Antibacterial Activity ◽  
Low Toxicity ◽  
New Compounds

As a continuation of our research and with the aim of obtaining new antibacterial agents which can improve the current chemotherapeutic antibacterial treatments, a series of quinoxaline-1,4-di-N-oxide derivatives were synthesized and evaluated for antibacterial activity against bacterial growing in macrophages in vitro. The results indicate that the new compounds exhibited a good antibacterial activity. Also, the potency and low toxicity of these compounds make them valid leads for synthesizing new compounds that possess better activity.

scholarly journals The Role of Supplementation with Natural Compounds in Post-Stroke Patients

2021 ◽  
Vol 22 (15) ◽  
pp. 7893
Author(s):  
Natalia Cichon ◽  
Joanna Saluk-Bijak ◽  
Elzbieta Miller ◽  
Leslaw Gorniak ◽  
Justyna Redlicka ◽  
...  
Keyword(s):  
Cerebral Stroke ◽  
Stroke Patients ◽  
Natural Origin ◽  
Post Stroke ◽  
Current State ◽  
Negative Prognostic Factor ◽  
Therapeutic Properties ◽  
New Compounds

Malnutrition is a serious problem in post-stroke patients. Importantly, it intensifies with hospitalization, and is related to both somatic and psychological reasons, as well as is associated with the insufficient knowledge of people who accompany the patient. Malnutrition is a negative prognostic factor, leading to a reduction in the quality of life. Moreover, this condition significantly extends hospitalization time, increases the frequency of treatment in intensive care units, and negatively affects the effectiveness of rehabilitation. Obtaining growing data on the therapeutic effectiveness of new compounds of natural origin is possible through the use of pharmacodynamic and analytical methods to assess their therapeutic properties. The proper supply of nutrients, as well as compounds of natural origin, is an important element of post-stroke therapy, due to their strong antioxidant, anti-inflammatory, neuroprotective and neuroplasticity enhancing properties. Taking the above into account, in this review we present the current state of knowledge on the benefits of using selected substances of natural origin in patients after cerebral stroke.

scholarly journals 1,2,4-Oxadiazole-Based Bio-Isosteres of Benzamides: Synthesis, Biological Activity and Toxicity to Zebrafish Embryo

2021 ◽  
Vol 22 (5) ◽  
pp. 2367
Author(s):  
Sen Yang ◽  
Chao-Li Ren ◽  
Tian-Yang Ma ◽  
Wen-Qian Zou ◽  
Li Dai ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antifungal Activity ◽  
Acute Toxicity ◽  
High Activity ◽  
Broad Spectrum ◽  
Zebrafish Embryo ◽  
Thanatephorus Cucumeris ◽  
Low Toxicity ◽  
New Compounds ◽  
Better Than

To discover new compounds with broad spectrum and high activity, we designed a series of novel benzamides containing 1,2,4-oxadiazole moiety by bioisosterism, and 28 benzamides derivatives with antifungal activity were synthesized. These compounds were evaluated against four fungi: Botrytis cinereal, FusaHum graminearum, Marssonina mali, and Thanatephorus cucumeris. The results indicated that most of the compounds displayed good fungicidal activities, especially against Botrytis cinereal. For example, 10a (84.4%), 10d (83.6%), 10e (83.3%), 10f (83.1%), 10i (83.3%), and 10l (83.6%) were better than pyraclostrobin (81.4%) at 100 mg/L. In addition, the acute toxicity of 10f to zebrafish embryo was 20.58 mg/L, which was classified as a low-toxicity compound.

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