Zeitschriftenartikel: „Azo compounds Toxicology“

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Sarah Mohammed Abed und Hasan Thamer Ghanem. „Synthesis and characterization Some of heterocyclic compounds from Nitrogen derivative“. International Journal of Research in Pharmaceutical Sciences 10, Nr. 4 (16.10.2019): 3186–96. http://dx.doi.org/10.26452/ijrps.v10i4.1621.

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This paper involves the synthesis of new oxazepine derivatives by multi-reaction steps. The first step synthesis azo derivative from 2-naphthol with 3-aminoacetophenone. The second step was the condensation reaction between ketone group of the azo compound and different primary aromatic amines (4-amino phenol, 3-nitro aniline and 4-methyl aniline) to yiled new azo Schiff base compounds (S1-S3) respectively. In the final step, Oxazepine compounds (L1-L3)and (L4-L6)were prepared from reaction imine compounds (S1-S3) with maleic and phthalic anhydride in toluene as solvent. All these derivatives were characterized by melting point, FTIR, HNMR and 13CNMR.

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Gadaleta, Domenico, Nicola Porta, Eleni Vrontaki, Serena Manganelli, Alberto Manganaro, Guido Sello, Masamitsu Honma und Emilio Benfenati. „Integrating computational methods to predict mutagenicity of aromatic azo compounds“. Journal of Environmental Science and Health, Part C 35, Nr. 4 (02.10.2017): 239–57. http://dx.doi.org/10.1080/10590501.2017.1391521.

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Tsuda, Shuji, Naonori Matsusaka, Hiroo Madarame, Shunji Ueno, Nobuyuki Susa, Kumiko Ishida, Noriko Kawamura, Kaoru Sekihashi und Yu F. Sasaki. „The comet assay in eight mouse organs: results with 24 azo compounds“. Mutation Research/Genetic Toxicology and Environmental Mutagenesis 465, Nr. 1-2 (Februar 2000): 11–26. http://dx.doi.org/10.1016/s1383-5718(99)00199-0.

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Weber, Eric J., und N. Lee Wolfe. „Kinetic studies of the reduction of aromatic AZO compounds in anaerobic sediment/water systems“. Environmental Toxicology and Chemistry 6, Nr. 12 (Dezember 1987): 911–19. http://dx.doi.org/10.1002/etc.5620061202.

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ELENA, PERDUM, MEDVEDOVICI ANDREI VALENTIN, TACHE FLORENTIN, VISILEANU EMILIA, DUMITRESCU IULIANA, MITRAN CORNELIA-ELENA, IORDACHE OVIDIU-GEORGE und RADULESCU ION RAZVAN. „Some validation aspects on the analytical method for assaying carcinogenic amines from textile dyes“. Industria Textila 69, Nr. 03 (01.07.2018): 249–56. http://dx.doi.org/10.35530/it.069.03.1521.

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Chemicals safety control and ecological properties have become a priority for the textile industry in order to avoid the negative effects on humans and environment. The increasing interest for toxicology of textiles is determined by the presence of dangerous compounds in clothes generated from dyeing and finishing processes. In order to protect human health, European Regulations as Oeko Tex Standard 100 and REACH Regulation limit the presence of dangerous chemicals, such as aromatic amines, generated by reductive cleavage of azo dyes, by no more than 30 mg/kg of textile material. The main goal of this research work was to develop and validate a HPLC/MWD method for precise and reliable identification and quantification of carcinogenic aromatic amines derived from banned azo dye specific to the textile industry. The simultaneous determination of 24 regulated aromatic amines has been conducted by two chromatographic methods according to SR EN ISO 14362-1:2017 in order to avoid matrix interferences and compounds misidentification due to the presence of structural isomers. Preliminary analyses to establish the maximum absorption wavelength of each standard solution of aromatic amine were performed simultaneously at four wavelengths, 240, 280, 305 and 380 nm. With the scope of demonstrating the consistency, reliability and accuracy of the analysed data, both liquid and gas chromatographic method were validated. Parameters as selectivity, precision, limit of detection and limit of quantification of the analytical methods were evaluated. The certainty of the determinations was also proved by the results of proficiency testing conducted by IIS Netherlands on azo dyes in textiles.

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Shao, Jie, Nicholas E. Geacintov und Vladimir Shafirovich. „Oxidation of 8-Oxo-7,8-dihydro-2′-deoxyguanosine by Oxyl Radicals Produced by Photolysis of Azo Compounds“. Chemical Research in Toxicology 23, Nr. 5 (17.05.2010): 933–38. http://dx.doi.org/10.1021/tx100022x.

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Rafii, F., und C. E. Cerniglia. „Reduction of azo dyes and nitroaromatic compounds by bacterial enzymes from the human intestinal tract.“ Environmental Health Perspectives 103, suppl 5 (Juni 1995): 17–19. http://dx.doi.org/10.1289/ehp.95103s417.

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Cox, Julie A., und Paul A. White. „The mutagenic activity of select azo compounds in MutaMouse target tissues in vivo and primary hepatocytes in vitro“. Mutation Research/Genetic Toxicology and Environmental Mutagenesis 844 (August 2019): 25–34. http://dx.doi.org/10.1016/j.mrgentox.2019.06.003.

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Li, Xue, und Yong-min Zhang. „Study on the reactions of azo compounds with acyl halides mediated by Sm/TiCl4“. Journal of Zhejiang University SCIENCE B 7, Nr. 3 (März 2006): 198–201. http://dx.doi.org/10.1631/jzus.2006.b0198.

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Telke, Amar A., Dayanand C. Kalyani, Vishal V. Dawkar und Sanjay P. Govindwar. „Influence of organic and inorganic compounds on oxidoreductive decolorization of sulfonated azo dye C.I. Reactive Orange 16“. Journal of Hazardous Materials 172, Nr. 1 (Dezember 2009): 298–309. http://dx.doi.org/10.1016/j.jhazmat.2009.07.008.

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Ong, Soon-An, Katsuhiro Uchiyama, Daisuke Inadama und Kazuaki Yamagiwa. „Simultaneous removal of color, organic compounds and nutrients in azo dye-containing wastewater using up-flow constructed wetland“. Journal of Hazardous Materials 165, Nr. 1-3 (15.06.2009): 696–703. http://dx.doi.org/10.1016/j.jhazmat.2008.10.071.

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Qin, Xing, Xiaoyun Su, Tao Tu, Jie Zhang, Xiaolu Wang, Yaru Wang, Yuan Wang et al. „Enzymatic Degradation of Multiple Major Mycotoxins by Dye-Decolorizing Peroxidase from Bacillus subtilis“. Toxins 13, Nr. 6 (19.06.2021): 429. http://dx.doi.org/10.3390/toxins13060429.

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The co-occurrence of multiple mycotoxins, including aflatoxin B1 (AFB1), zearalenone (ZEN) and deoxynivalenol (DON), widely exists in cereal-based animal feed and food. At present, most reported mycotoxins degrading enzymes target only a certain type of mycotoxins. Therefore, it is of great significance for mining enzymes involved in the simultaneous degradation of different types of mycotoxins. In this study, a dye-decolorizing peroxidase-encoding gene BsDyP from Bacillus subtilis SCK6 was cloned and expressed in Escherichia coli BL21/pG-Tf2. The purified recombinant BsDyP was capable of oxidizing various substrates, including lignin phenolic model compounds 2,6-dimethylphenol and guaiacol, the substrate 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid), anthraquinone dye reactive blue 19 and azo dye reactive black 5, as well as Mn2+. In addition, BsDyP could efficiently degrade different types of mycotoxins, including AFB1, ZEN and DON, in presence of Mn2+. More important, the toxicities of their corresponding enzymatic degradation products AFB1-diol, 15-OH-ZEN and C15H18O8 were significantly lower than AFB1, ZEN and DON. In summary, these results proved that BsDyP was a promising candidate for the simultaneous degradation of multiple mycotoxins in animal feed and food.

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Manahil B Elamin, Amani Abd Elrazig Salman Abd Elaziz und Emad Mohamed Abdallah. „Benzothiazole moieties and their derivatives as antimicrobial and antiviral agents: A mini-review“. International Journal of Research in Pharmaceutical Sciences 11, Nr. 3 (08.07.2020): 3309–15. http://dx.doi.org/10.26452/ijrps.v11i3.2459.

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Heterocyclic chemistry has provided an inexhaustible source of pharmaceutical molecules. Heterocyclic compounds such as benzothiazole moieties and its derivatives area substantial class of compounds in pharmaceutical chemistry and exhibited therapeutic capabilities, such as antitumor, anticancer, antioxidant, antidiabetic, antiviral, antimicrobial, antimalarial, anthelmintic and other activities. Besides, some antibiotics such as penicillin and cephalosporin have heterocyclic moiety. The growing prevalence of multi-drug resistant pathogens represents serious global concern,which requires the development of new antimicrobial drugs. Moreover, the emergence of pandemic SARSCoV-2 causing Covid-19 disease and all these health dilemmas urge the scientific community to examine the possible antimicrobial and antiviral capacities of some bioactive benzothiazole derivatives against these severe causative agents.This mini-review highlights some recent scientific literature on different benzothiazole molecules and their derivatives. It turns out that, there are numerous synthesized benzothiazole derivatives which exhibited different mode of actions against microorganisms or viruses and accordingly suggested them as an active candidate in the discovery of new antimicrobial or antiviral agents for clinical development. The recommended bioactive benzothiazole derivatives mentioned in the current study are mainly Schiff bases, azo dyes and metal complexes benzothiazole derivatives; the starting material for most of these derivatives are 2-aminobenzothiazole although careful pharmaceutical studies should be conducted to ensure the safety and efficacy of these bioactive synthesized molecules as an antimicrobial or antiviral drug in the future.

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Luo, Yiqi Ruben, Cassandra Yun und Kara L. Lynch. „Quantitation of Cannabinoids in Breath Samples Using a Novel Derivatization LC–MS/MS Assay with Ultra-High Sensitivity“. Journal of Analytical Toxicology 43, Nr. 5 (05.04.2019): 331–39. http://dx.doi.org/10.1093/jat/bkz023.

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Abstract As the legalization of medical and recreational marijuana use expands, measurement of tetrahydrocannabinol (THC) in human breath has become an area of interest. The presence and concentration of cannabinoids in breath have been shown to correlate with recent marijuana use and may be correlated with impairment. Given the low concentration of THC in human breath, sensitive analytical methods are required to further evaluate its utility and window of detection. This paper describes a novel derivatization method based on an azo coupling reaction that significantly increases the ionization efficiency of cannabinoids for LC–MS/MS analysis. This derivatization reaction allows for a direct derivatization reaction with neat samples and does not require further sample clean-up after derivatization, thus facilitating an easy and rapid “derivatize & shoot” sample preparation. The derivatization assay allowed for limits of quantitation (LOQ’s) in the sub-pg/mL to pg/mL range for the five cannabinoids in breath samples, i.e., only 5~50 femtograms of an analyte was required for quantitation in a single analysis. This ultrahigh sensitivity allowed for the quantitation of cannabinoids in all breath samples collected within 3 hours of smoking cannabis (n = 180). A linear correlation between THC and cannabinol (CBN) in human breath was observed, supporting the hypothesis that CBN is converted from THC during the combustion of cannabis. The derivatization method was also applied to the analysis of cannabinoids in whole blood samples, achieving LOQ’s at ten-pg/mL to sub-ng/mL level. This azo coupling-based derivatization approach provided the needed analytical sensitivity for the analysis of THC in human breath samples using LC–MS/MS and could be a valuable tool for the analysis of other aromatic compounds in the future.

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Francesconi, Kevin A. „Arsenic species in seafood: Origin and human health implications“. Pure and Applied Chemistry 82, Nr. 2 (16.01.2010): 373–81. http://dx.doi.org/10.1351/pac-con-09-07-01.

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The presence of arsenic in marine samples was first reported over 100 years ago, and shortly thereafter it was shown that common seafood such as fish, crustaceans, and molluscs contained arsenic at exceedingly high concentrations. It was noted at the time that this seafood arsenic was probably present as an organically bound species because the concentrations were so high that if the arsenic had been present as an inorganic species it would certainly have been toxic to the humans consuming seafood. Investigations in the late 1970s identified the major form of seafood arsenic as arsenobetaine [(CH3)3As+CH2COO–], a harmless organoarsenic compound which, following ingestion by humans, is rapidly excreted in the urine. Since that work, however, over 50 additional arsenic species have been identified in marine organisms, including many important food products. For most of these arsenic compounds, the human toxicology remains unknown. The current status of arsenic in seafood will be discussed in terms of the possible origin of these compounds and the implications of their presence in our foods.

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Kurochka, Andrey V., Ol'ga V. Agafonova, Aleksandr S. Losev, Elizaveta A. Mamaeva, Sergey Yu Bylikin, Vadim V. Negrebetsky, Evgeniya P. Kramarova, Aleksandr G. Shipov und Yuri I. Baukov. „Six- and Seven-Membered 1-Oxa-4-Aza-2-Silacyclanes as Possible Correctors of Adaptational Mechanisms“. Metal-Based Drugs 5, Nr. 1 (01.01.1998): 25–33. http://dx.doi.org/10.1155/mbd.1998.25.

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The biological activity of eight 1-oxa-4-aza-2-silacyclanes with the OSiCH2N fragment including 6-membered 2-sila-5-morpholinones (1–3) and 4-acyl-2-silamorpholines (4–6)and previously unknown 7-membered derivatives of salicylic acid (7, 8) was studied. Compounds 1 and 3–6 show the certain antihypoxic action. Compounds 2 (40 mg/kg), 4 (20 mg/kg), 6 (40 mg/kg), 7 (20 mg/kg) and 8 (40 mg/kg) reduce the physical serviceability of intact animals. Compound 1 (20 mg/kg) influences the physical serviceability in a moderate-positive way on the background of chlorophos-poisoning. Compounds 5–8 displayed protective properties against chlorophos-poisoning at the LD50 dose and compounds 2, 4, 5, 7 at the LD100 dose. Influence of compounds 1 and 2 on the emotional-research behavior of mice was studied.

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Kitada, Shinichi, Christina L. Kress, Maryla Krajewska, Lee Jia, Maurizio Pellecchia und John C. Reed. „Bcl-2 antagonist apogossypol (NSC736630) displays single-agent activity in Bcl-2–transgenic mice and has superior efficacy with less toxicity compared with gossypol (NSC19048)“. Blood 111, Nr. 6 (15.03.2008): 3211–19. http://dx.doi.org/10.1182/blood-2007-09-113647.

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Abstract Altered expression of Bcl-2 family proteins plays central roles in apoptosis dysregulation in cancer and leukemia, promoting malignant cell expansion and contributing to chemoresistance. In this study, we compared the toxicity and efficacy in mice of natural product gossypol and its semisynthetic derivative apo-gossypol, compounds that bind and inhibit antiapoptotic Bcl-2 family proteins. Daily oral dosing studies showed that mice tolerate doses of apogossypol 2- to 4-times higher than gossypol. Hepatotoxicity and gastrointestinal toxicity represented the major adverse activities of gossypol, with apogossypol far less toxic. Efficacy was tested in transgenic mice in which Bcl-2 is overexpressed in B cells, resembling low-grade follicular lymphoma in humans. In vitro, Bcl-2–expressing B cells from transgenic mice were more sensitive to cytotoxicity induced by apogossypol than gossypol, with LD50 values of 3 to 5 μM and 7.5 to 10 μM, respectively. In vivo, using the maximum tolerated dose of gossypol for sequential daily dosing, apogossypol displayed superior activity to gossypol in terms of reducing splenomegaly and reducing B-cell counts in spleens of Bcl-2–transgenic mice. Taken together, these studies indicate that apogossypol is superior to parent compound gossypol with respect to toxicology and efficacy, suggesting that further development of this compound for cancer therapy is warranted.

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Newman, L. M., R. L. Giacobbe, L.-J. Fu und E. M. Johnson. „Developmental Toxicity Evaluation of Several Cosmetic Ingredients in the Hydra Assay“. Journal of the American College of Toxicology 9, Nr. 3 (Mai 1990): 361–65. http://dx.doi.org/10.3109/10915819009078745.

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The developmental toxicity hazard potential of six cosmetic products was determined in the in vitro Hydra assay. These studies were conducted to supplement available toxicological information and provide an indication of the priority of these compounds for higher level (in vivo) developmental toxicity testing. All but one ingredient, potassium sorbate, was predicted by the assay to be generally equally or more toxic to adults than to embryos and, therefore, to be low-priority chemicals for more elaborate tests. In contrast, assay results suggest that potassium sorbate is a prime candidate for higher-level animal developmental toxicology testing. The endpoints for this in vitro prescreen were ‘set’ some years ago to avoid false negatives as much as possible, but approximately 7% false positives result. Therefore, it is premature to consider sorbate as being uniquely hazardous to in utero development until this is established by testing in pregnant laboratory mammals.

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Hijaz, Faraj, und Nabil Killiny. „Evaluation of Oxytetracycline Metabolites Cross-Reactivity with Oxytetracycline Enzyme-Linked Immunosorbent Assay (ELISA)“. Antibiotics 9, Nr. 4 (15.04.2020): 183. http://dx.doi.org/10.3390/antibiotics9040183.

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Antibiotics have been successfully used for the control of several plant diseases for many years. Recently, streptomycin and oxytetracycline have been approved for the treatment of Huanglongbing (HLB) in Florida. The enzyme-linked immunosorbent assay (ELISA) is the most commonly used assay for the detection of these antibiotics because it is quick, simple, and can be used to analyze many samples at the same time. However, ELISA can react with the metabolites of the parent compound and its structurally related compounds. In this study, we investigated the cross-reactivity of the oxytetracycline ACCEL ELISA kitTM with three of oxytetracycline metabolites (4-epi-oxytetracycline, α-apo-oxytetracycline, and β-apo-oxytetracycline). The α-apo-oxytetracycline and β-apo-oxytetracycline metabolite did not show any cross-reactivity in the linear range (1.5–50 ng mL−1) of the assay. Whereas 4-epi-oxytetracycline showed high cross-reactivity, and its response was similar to oxytetracycline. Our results indicated that the oxytetracycline ELISA kits estimate the level of oxytetracycline as well as its main metabolite, 4-epi-oxytetracycline.

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Hubbs, Ann F., Kathleen Kreiss, Kristin J. Cummings, Kara L. Fluharty, Ryan O’Connell, Allison Cole, Tiana M. Dodd et al. „Flavorings-Related Lung Disease: A Brief Review and New Mechanistic Data“. Toxicologic Pathology 47, Nr. 8 (23.10.2019): 1012–26. http://dx.doi.org/10.1177/0192623319879906.

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Flavorings-related lung disease is a potentially disabling and sometimes fatal lung disease of workers making or using flavorings. First identified almost 20 years ago in microwave popcorn workers exposed to butter-flavoring vapors, flavorings-related lung disease remains a concern today. In some cases, workers develop bronchiolitis obliterans, a severe form of fixed airways disease. Affected workers have been reported in microwave popcorn, flavorings, and coffee production workplaces. Volatile α-dicarbonyl compounds, particularly diacetyl (2,3-butanedione) and 2,3-pentanedione, are implicated in the etiology. Published studies on diacetyl and 2,3-pentanedione document their ability to cause airway epithelial necrosis, damage biological molecules, and perturb protein homeostasis. With chronic exposure in rats, they produce airway fibrosis resembling bronchiolitis obliterans. To add to this knowledge, we recently evaluated airway toxicity of the 3-carbon α-dicarbonyl compound, methylglyoxal. Methylglyoxal inhalation causes epithelial necrosis at even lower concentrations than diacetyl. In addition, we investigated airway toxicity of mixtures of diacetyl, acetoin, and acetic acid, common volatiles in butter flavoring. At ratios comparable to workplace scenarios, the mixtures or diacetyl alone, but not acetic acid or acetoin, cause airway epithelial necrosis. These new findings add to existing data to implicate α-dicarbonyl compounds in airway injury and flavorings-related lung disease.

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Zhu, Jianyu, Jeffrey Meeusen, Susan Krezoski und David H. Petering. „Reactivity of Zn-, Cd-, and Apo-Metallothionein with Nitric Oxide Compounds: In Vitro and Cellular Comparison“. Chemical Research in Toxicology 23, Nr. 2 (15.02.2010): 422–31. http://dx.doi.org/10.1021/tx900387k.

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Ye, Yuerong, Colin C. Duke und Gerald M. Holder. „Identification of Hepatic Metabolites of Two Highly Carcinogenic Polycyclic Aza-Aromatic Compounds, 7,9-Dimethylbenz[c]acridine and 7,10-Dimethylbenz[c]acridine“. Chemical Research in Toxicology 8, Nr. 2 (März 1995): 188–202. http://dx.doi.org/10.1021/tx00044a003.

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Cervantes, G., V. Moreno, E. Molins und C. Miravitlles. „Reactions of Pd(II) and Pt(II) Complexes With Tetraethylthiouram Disulfide“. Metal-Based Drugs 4, Nr. 6 (01.01.1997): 317–25. http://dx.doi.org/10.1155/mbd.1997.317.

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The reactions of tetraethylthiouram disulfide (DTS), an inhibitor of the nephrotoxicity of Pt(II) drugs, an efficient agent in the treatment of chronic alcoholism, in the treatment of HIV infections, AIDS and heavy metal toxicity, and a fungicide and herbicide, with K2[PtCl4], in ratio 1:1 and 1:2, gave the compounds [PtCl2DTS] and [Pt(S2CNEt2)2] respectively. The reaction of the complexes K2[PdCl4], Pd(AcO)2 and [PdCl2(PhCN)2], where PhCN = Benzonitrile, with tetraethylthiouram disulfide in ratio 1:1 or 1:2, yielded orange crystals identified as [Pd(S2CNEt2)2]. The crystals were suitable for study by X-ray diffraction. The -S-S- bridge in the tetraethylthiouram disulfude molecule was broken and the two molecules of the thiocarbamate derivative were bound to the Pd(II) by the equivalents sulfur atoms. All the compounds were characterized by IR, H1 and C13 NMR spectroscopies.

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Vedika Dadlani, Pushpendra Tripathi und Rakesh Somani. „Design, Molecular Docking and In-Silico Analysis of Novel thiadiazole-azetidinone hybrids as Potential Antitubercular Agents“. International Journal of Research in Pharmaceutical Sciences 10, Nr. 4 (29.11.2019): 3694–703. http://dx.doi.org/10.26452/ijrps.v10i4.1756.

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The recent emergence of extensively drug-resistant tuberculosis has become a cause of concern for the management of tuberculosis globally. Shikimic acid pathway seems to be a potential and favorable target for the drug design of new anti-infective agents. This work aims to change the focus from traditional cell approaches to the target-based design of novel thiadiazolyl-azetidinone derivatives with Shikimate kinase as the drug target for anti-tubercular activity. Thiadiazole and azetidinone derivatives were methodically reprised to design a series of 3-chloro-4-(aryl)-1-(5-sulfanyl-1,3,4-thiadiazol-2-yl)azetidin-2-one derivatives (AZ1-AZ12). Molecular docking studies were performed on a crystal model of Mycobacterium tuberculosis Shikimate kinase (MtSK) using Vlife MDS 4.4 suite to evaluate their anti-tubercular potential. Further, drug-likeness properties and ADMET prediction were performed by molinspiration and admetSAR software to better describe the designed molecules as prospective candidates. 3-chloro-4-(4-nitrophenyl)-1-(5-sulfanyl-1,3,4-thiadiazol-2-yl)azetidin-2-one (AZ3), was found to be have better dock score when compared with the natural substrate, Shikimate. Docking studies confirmed that the molecules showed significant binding in the active site region of Shikimate kinase. Strong hydrogen bonding and hydrophobic interactions with amino acid residues and other parameters further explicate their effectiveness for inhibition of MtSK. Also, the physicochemical properties and drug scores for the designed compounds obtained by in silico studies were found to be satisfactory, signifying the overall potential of the designed molecules to be drug candidates. Thus these molecules could be explored as a lead for further anti-tubercular studies with Mycobacterium tuberculosis Shikimate kinase as the drug target.

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Shah, Syed Muhammad Ali, Muhammad Akram, Muhammad Riaz, Naveed Munir und Ghulam Rasool. „Cardioprotective Potential of Plant-Derived Molecules: A Scientific and Medicinal Approach“. Dose-Response 17, Nr. 2 (01.04.2019): 155932581985224. http://dx.doi.org/10.1177/1559325819852243.

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Since the beginning of human civilization, plants have been used in alleviating the human distress and it was recorded for about thousands of years ago that the plants are being used for medicinal purposes. Natural bioactive compounds called phytochemicals are obtained from medicinal plants, vegetables, and fruits, which functions to combat against various ailments. There is dire need to explore the plant biodiversity for its medicinal and pharmacological potentials. Different databases such as Google scholar, Medline, PubMed, and the Directory of Open Access Journals were searched to find the articles describing the cardioprotective function of medicinal plants. Various substances from a variety of plant species are used for the treatment of cardiovascular abnormalities. The cardioprotective plants contain a variety of bioactive compounds, including diosgenin, isoflavones, sulforaphane, carotinized, catechin, and quercetin, have been proved to enhance cardioprotection, hence reducing the risk of cardiac abnormalities. The present review article provides the data on the use of medicinal plants particularly against cardiac diseases and to explore the molecules/phytoconstituents as plant secondary metabolites for their cardioprotective potential.

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Karadag, AS, M. Kavala, FT Demir, Z. Turkoğlu, İ. Kartal und E. Zemheri. „A case of hyperpigmentation and acanthosis nigricans by testosterone injections“. Human & Experimental Toxicology 33, Nr. 12 (06.02.2014): 1297–301. http://dx.doi.org/10.1177/0960327113514099.

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Drug-related skin disorders may occur in many different ways. Despite pigmentary changes being less important for morbidity, these changes precipitate depressed mood and reduce self-confidence. Testosterone is a steroid hormone from the androgen group and primarily used for the treatment of hypogonadism in males. Testosterone replacement can cause skin problems like acne, hair loss, redness, pain, or infection at the injection site. The study was conducted on a 49-year-old man with adult onset idiopathic hypogonadotropic hypogonadism, which is an acquired form of isolated gonadotropin-releasing hormone deficiency. He was presented with lack of energy and decreased sexual function 10 years ago and was given an oil-based injectable blend of four esterized testosterone compounds as hormone replacement treatment in a urology polyclinic. He was referred to our polyclinic by endocrinologist because of progressive hyperpigmentation marked on his face and oral mucosa. In the present study, we report the first testosterone therapy-related facial and oral mucosal hyperpigmentation and acanthosis nigricans in the same patient.

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Barreiro, Carlos, Juan F. Martín und Carlos García-Estrada. „Proteomics Shows New Faces for the Old Penicillin ProducerPenicillium chrysogenum“. Journal of Biomedicine and Biotechnology 2012 (2012): 1–15. http://dx.doi.org/10.1155/2012/105109.

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Fungi comprise a vast group of microorganisms including the Ascomycota (majority of all described fungi), the Basidiomycota (mushrooms or higher fungi), and the Zygomycota and Chytridiomycota (basal or lower fungi) that produce industrially interesting secondary metabolites, such as β-lactam antibiotics. These compounds are one of the most commonly prescribed drugs world-wide. Since Fleming's initial discovery ofPenicillium notatum80 years ago, the role ofPenicilliumas an antimicrobial source became patent. After the isolation ofPenicillium chrysogenumNRRL 1951 six decades ago, classical mutagenesis and screening programs led to the development of industrial strains with increased productivity (at least three orders of magnitude). The new “omics” era has provided the key to understand the underlying mechanisms of the industrial strain improvement process. The review of different proteomics methods applied toP. chrysogenumhas revealed that industrial modification of this microorganism was a consequence of a careful rebalancing of several metabolic pathways. In addition, the secretome analysis ofP. chrysogenumhas opened the door to new industrial applications for this versatile filamentous fungus.

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Duringer, Jennifer, Rajarshi Mazumder, Valerie Palmer, A. Morrie Craig und Peter Spencer. „Case-Control Study of Nodding Syndrome in Acholiland: Urinary Multi-Mycotoxin Screening“. Toxins 13, Nr. 5 (27.04.2021): 313. http://dx.doi.org/10.3390/toxins13050313.

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This case-control study adds to the growing body of knowledge on the medical, nutritional, and environmental factors associated with Nodding Syndrome (NS), a seizure disorder of children and adolescents in northern Uganda. Past research described a significant association between NS and prior history of measles infection, dependence on emergency food and, at head nodding onset, subsistence on moldy maize, which has the potential to harbor mycotoxins. We used LC-MS/MS to screen for current mycotoxin loads by evaluating nine analytes in urine samples from age-and-gender matched NS cases (n = 50) and Community Controls (CC, n = 50). The presence of the three mycotoxins identified in the screening was not significantly different between the two groups, so samples were combined to generate an overall view of exposure in this community during the study. Compared against subsequently run standards, α-zearalenol (43 ± 103 µg/L in 15 samples > limit of quantitation (LOQ); 0 (0/359) µg/L), T-2 toxin (39 ± 81 µg/L in 72 samples > LOQ; 0 (0/425) µg/L) and aflatoxin M1 (4 ± 10 µg/L in 15 samples > LOQ; 0 (0/45) µg/L) were detected and calculated as the average concentration ± SD; median (min/max). Ninety-five percent of the samples had at least one urinary mycotoxin; 87% were positive for two of the three compounds detected. While mycotoxin loads at NS onset years ago are and will remain unknown, this study showed that children with and without NS currently harbor foodborne mycotoxins, including those associated with maize.

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Khawla Salman Abd-Alrassol, Qutaiba A. Qasim, Maitham Ali AL-Rikabi und H. N. K. AL-Salman. „The development of analytical methods to determine metoclopramide-hydrochloric acid in the standard raw and it compared with pharmaceuticals“. International Journal of Research in Pharmaceutical Sciences 10, Nr. 4 (05.11.2019): 3461–74. http://dx.doi.org/10.26452/ijrps.v10i4.1663.

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The three novel easy, to the prepare and sensitive spectral methods, were used to estimate metoclopramide in both standard and pharmaceuticals. The effective double–electron, was present in the metoclopramide compound helps to interact in an acidic medium with a reagent such as diazetide resorcinol and 8-hydroxyquinoline reagents. The present article was extended to find out three analytical methods with UV-V is the detector. In both A and B methods, two azo-dyes are formed, they are orange-red and red stable and have high water solubility, giving highest absorption values at 415 nm and 485 nm but the C method will depend on a complex colour configuration with the p-benzoquinone reagent, which has a maximum absorption at a wavelength of 285 nm. Beer's law was applied in a range of concentrations between 1 and 10 μg / ml, 2-20 μg / ml and 1-30 μg / ml. The values of the molar absorption factors were (4.1224 × 104, 3.0229 × 104 and 1.7373 × 104) L mol-1cm-1 with a sensitivity of Sandell’s equal to 0.2606 × 10-4, 0.9834 × 10-4 and 0.2568 × 10 - 4 μg cm-2 to methods A, B respectively and LLOD values were 0.255, 0.553 and 0.158 μg / ml to methods A, B and C. LLOQ 0.512, 0.898 and 0.455 μg / ml to methods A, B, C respectively. The constant fixed Kf configuration was also calculated for the colored outputs of the reaction where it was found to be equal to 43.6435 × 108, 54.6261 × 10-8 and 17.29099 × 106 L2 mol-2 to all methods A, B, C respectively. The values of G were calculated based on -43.9293 KJ / mol, -44.3735 and -51.2019. G values, molar absorption factor, Sandell sensitivity, detection limit.

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Sips, Luc, Emmanuel Njumbe Ediage, Benno Ingelse, Tom Verhaeghe und Lieve Dillen. „LC–MS quantification of oligonucleotides in biological matrices with SPE or hybridization extraction“. Bioanalysis 11, Nr. 21 (November 2019): 1941–54. http://dx.doi.org/10.4155/bio-2019-0117.

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Aim: Quantitative LC–MS analysis of oligonucleotides (OGNs) in biological matrices is needed to support candidate selection of new therapeutic OGNs. Methodology & results: A set of 20 single stranded antisense oligonucleotides (ASO) and five siRNAs were extracted from plasma and tissue homogenates. Anion Exchange (AEX) SPE was selected as generic extraction approach, resulting in recoveries from plasma >70%. Extraction from tissue homogenates showed often more variation and lower recoveries. A proof of concept of a novel tailored hybridization extraction is demonstrated for two 16-mer reference OGNs. Conclusion: Two methods for extraction of OGNs were investigated and applied for quantitative analysis. The AEX-SPE is considered a more generic approach preferred when multiple compounds are evaluated. Hybridization extraction has great potential but critical reagents per analyte are needed.

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Singh, P., B. Morris, S. Zhao und B. L. Blaylock. „Suppression of the Contact Hypersensitivity Response Following Topical Exposure to 2-Butoxyethanol in Female BALB/c Mice“. International Journal of Toxicology 21, Nr. 2 (März 2002): 107–14. http://dx.doi.org/10.1080/10915810252866088.

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The effects of route of exposure, time of exposure and metabolism of 2-butoxyethanol (BE) on the contact hypersensitivity response (CHR) were evaluated in female BALB/c mice. Mice were either orally exposed to 50, 150 or 400 mg BE/kg or topically exposed to 0.25, 1.0, 4.0 or 16.0 mg BE on the ear and the oxazolone (OXA)-induced CHR evaluated by measuring ear thickness before and after OXA challenge. While no modulation was observed following oral exposure to BE, topical exposure resulted in a significant decrease in the CHR. Application of 4.0 mg BE in 4:1 acetone and olive oil (AOO) vehicle at the time of sensitization, challenge or both, decreased the CHR by 18%, 18% and 22%, respectively. A time course study of the effects of topical exposure to 4.0 mg BE/ear during the challenge phase of the CHR revealed that BE must be applied at the time of OXA challenge to significantly reduce the ear swelling response. In order to determine if metabolism of topically applied BE was required for suppression of the CHR, butoxyacetic acid (BAA), the primary metabolite of BE, was applied to the ear immediately following OXA challenge. No topical dose of BAA (2.0, 4.0 and 8.0 mg BAA/ear) administered in this study altered the CHR. Blocking the metabolism of BE by oral administration of 4-methylpyrazole (MP), further reduced OXA-induced ear swelling when compared to mice exposed to BE without MP treatment. Taken together, these studies indicated that suppression of the CHR in mice following topical exposure to this glycol ether was due to the activity of BE itself and was not dependent on metabolic activation of the compound. Further studies were undertaken to identify a potential mechanism of BE-induced reduction of the CHR. Epidermal cells from untreated BALB/c mice were isolated and exposed to BE in vitro (10–12, 10–10, 10–8, 10–6 and 10–4 M BE). In vitro exposure to BE at these concentrations did not significantly affect expression of MHC class II surface protein or protein synthesis in epidermal Langerhans cells, failing to provide in vitro evidence that BE-associated suppression of the CHR is associated with a reduction in MHC class II expression.

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Bagdonienė, Lida, Danutė Labeikytė, Ivars Kalviņš, Veronika Borutinskaitė, Aleksandrs Prokofjevs, Pēteris Trapencieris, Benediktas Juodka und Nikolajs Sjakste. „Rat Serum Carboxylesterase Partly Hydrolyses Gamma-Butyrobetaine Esters“. Archives of Industrial Hygiene and Toxicology 60, Nr. 2 (01.06.2009): 147–56. http://dx.doi.org/10.2478/10004-1254-60-2009-1915.

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Rat Serum Carboxylesterase Partly Hydrolyses Gamma-Butyrobetaine EstersAlthough described some time ago, gamma-butyrobetaine esters and related compounds have not gained much attention from researchers, and their physiological function remains obscure. Formerly we detected GBB-esterase enzymatic activity in rat blood serum using phenylated gamma-butyrobetaine as an artificial substrate of the enzyme and HPLC. The aim of the present work was to develop an assay that would enable spectrophotometric or colorimetric determination of the reaction products of GBB-esterase activity and to reveal individual proteins performing GBB-esterase activity in rat blood serum. For this purpose gamma-butyrobetaine 1-naphthyl ester was synthesised. Hydrolysis of this ester releases 1-naphthol, which increases the optical absorbance at 322 nm. We have shown that the enzymatic hydrolysis of GBB 1-naphthyl ester to 1-naphthol in rat blood serum is due to GBB-esterase activity. An attempt was done to purify the enzyme from rat blood serum. By combining DEAE Sepharose at pH 4.2 and affinity chromatography with procainamide we achieved a 68-fold enrichment of GBB-esterase activity in our preparations. Separation of fraction proteins in 2D protein electrophoresis with following mass-spectrometry indicated that GBB esterase activity in rat blood serum is performed in part by carboxylesterase.

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Romero-Palomo, Fernando, Matthias Festag, Barbara Lenz, Simone Schadt, Andreas Brink, Anja Kipar, Bernd Steinhuber et al. „Safety, Tissue Distribution, and Metabolism of LNA-Containing Antisense Oligonucleotides in Rats“. Toxicologic Pathology 49, Nr. 6 (01.06.2021): 1174–92. http://dx.doi.org/10.1177/01926233211011615.

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Antisense oligonucleotides (ASOs) are chemically modified nucleic acids with therapeutic potential, some of which have been approved for marketing. We performed a study in rats to investigate mechanisms of toxicity after administration of 3 tool locked nucleic acid (LNA)-containing ASOs with differing established safety profiles. Four male rats per group were dosed once, 3, or 6 times subcutaneously, with 7 days between dosing, and sacrificed 3 days after the last dose. These ASOs were either unconjugated (naked) or conjugated with N-acetylgalactosamine for hepatocyte-targeted delivery. The main readouts were in-life monitoring, clinical and anatomic pathology, exposure assessment and metabolite identification in liver and kidney by liquid chromatography coupled to tandem mass spectrometry, ASO detection in liver and kidney by immunohistochemistry, in situ hybridization, immune electron microscopy, and matrix-assisted laser desorption/ionization mass spectrometry imaging. The highly toxic compounds showed the greatest amount of metabolites and a low degree of tissue accumulation. This study reveals different patterns of cell death associated with toxicity in liver (apoptosis and necrosis) and kidney (necrosis only) and provides new ultrastructural insights on the tissue accumulation of ASOs. We observed that the immunostimulatory properties of ASOs can be either primary from sequence-dependent properties or secondary to cell necrosis.

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Marwal, Avinash, Mukesh Meena und RK Gaur. „Molecular Docking Studies of Coronavirus Proteins with Medicinal Plant Based Phytochemicals“. Defence Life Science Journal 6, Nr. 1 (23.02.2021): 57–63. http://dx.doi.org/10.14429/dlsj.6.15704.

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In this study, we presented an in silico molecular docking between the SARS-CoV-2 four proteins [(a) SARS-CoV-2 nucleocapsid protein N-terminal RNA binding domain (6M3M), (b) Nsp9 RNA binding protein of SARS CoV-2 (6W4B), (c) The crystal structure of COVID-19 main protease in apo form (6M03), and (d) Structure of the 2019-nCoV HR2 Domain (6LVN)] available in the PDB (Protein Data Bank), and the medicinal plant-based phytochemicals (retrieved from PubChem database) as ligand molecules i.e. Piperine (Black Pepper), Eugenol (Clove), Alliin (Garlic), Gingerol (Ginger) and Curcumin (Turmeric). All these ligand molecules showed good docking with their respective receptor molecules and their scores range from -8.195 to -5.263. DockThor Portal (a receptor ligand-docking server) which was recently developed and published this year were used in the current study. The obtained results might help in the wet lab conditions to develop better antiviral compounds against SARS-CoV-2.

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Hijaz, Faraj, Yasser Nehela, Pedro Gonzalez-Blanco und Nabil Killiny. „Development of Europium-Sensitized Fluorescence-Based Method for Sensitive Detection of Oxytetracycline in Citrus Tissues“. Antibiotics 10, Nr. 2 (23.02.2021): 224. http://dx.doi.org/10.3390/antibiotics10020224.

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Antimicrobial compounds have been successfully used to control many plant and animal diseases. Recently, oxytetracycline (OTC) and streptomycin have been approved for the treatment of Huanglongbing in citrus. Since the application of OTC is under strict regulations, several methods have been developed to determine and monitor its levels in the environment including high-performance liquid chromatography, ELISA, colorimetric, and fluorometric assays. In this study, we developed a fluorometric method for the determination of OTC in plant tissues based on its complexation with europium. Our preliminary trials showed that phenols and flavonoids interfere with the europium assay by reacting with the sensitizing reagent, cetyltrimethylammonium chloride. Consequently, we used the 60 mg hydrophilic–lipophilic balanced (HLB) cartridges to purify the OTC from the plant matrix. The recovery of OTC from spiked leaf samples was 75 ± 7.6%. Using the 500 mg HLB, we were able to detect 0.3 ppm OTC in the final sample extract, which corresponds to 3 µg g−1 fresh weight (FWT). The developed method was successfully used to measure the level of OTC in leaves obtained from trunk-injected trees. The results obtained by the europium method were similar to those obtained using the ELISA assay. We also tested the cross-reactivity of OTC metabolites with the europium method. The 4-epi-OTC showed a high cross-reactivity (50.0 ± 3.6%) with europium assay, whereas α-apo-OTC and β-apo-OTC showed small cross-reactivity. We showed that the europium-sensitized fluorescence-based method can be successfully used to assess OTC in citrus plant tissues after a cleanup step. Our results showed that this method was sensitive, reproducible, and can be used to analyze many samples simultaneously.

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Iseppi, Ramona, Martina Mariani, Carla Condò, Carla Sabia und Patrizia Messi. „Essential Oils: A Natural Weapon against Antibiotic-Resistant Bacteria Responsible for Nosocomial Infections“. Antibiotics 10, Nr. 4 (10.04.2021): 417. http://dx.doi.org/10.3390/antibiotics10040417.

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The emergence of antibiotic-resistant bacteria has become a major concern worldwide. This trend indicates the need for alternative agents to antibiotics, such as natural compounds of plant origin. Using agar disc diffusion and minimum inhibitory concentration (MIC) assays, we investigated the antimicrobial activity of Citrus aurantium (AEO), Citrus x limon (LEO), Eucalyptus globulus (EEO), Melaleuca alternifolia (TTO), and Cupressus sempervirens (CEO) essential oils (EOs) against three representatives of antibiotic-resistant pathogens and respective biofilms: vancomycin-resistant enterococci (VRE), methicillin-resistant Staphylococcus aureus (MRSA), and extended-spectrum β-lactamase (ESBL)-producing Escherichia coli. Using the checkerboard method, the efficacy of the EOs alone, in an association with each other, or in combination with the reference antibiotics was quantified by calculating fractional inhibitory concentrations (FICs). All the EOs displayed antibacterial activity against all strains to different extents, and TTO was the most effective. The results of the EO–EO associations and EO–antibiotic combinations clearly showed a synergistic outcome in most tests. Lastly, the effectiveness of EOs both alone and in association or combination against biofilm formed by the antibiotic-resistant strains was comparable to, and sometimes better than, that of the reference antibiotics. In conclusion, the combination of EOs and antibiotics represents a promising therapeutic strategy against antibiotic-resistant bacteria, even protected inside biofilms, which can allow decreasing the concentrations of antibiotics used.

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McLean, Thomas C., Barrie Wilkinson, Matthew I. Hutchings und Rebecca Devine. „Dissolution of the Disparate: Co-ordinate Regulation in Antibiotic Biosynthesis“. Antibiotics 8, Nr. 2 (18.06.2019): 83. http://dx.doi.org/10.3390/antibiotics8020083.

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Discovering new antibiotics is vital to combat the growing threat of antimicrobial resistance. Most currently used antibiotics originate from the natural products of actinomycete bacteria, particularly Streptomyces species, that were discovered over 60 years ago. However, genome sequencing has revealed that most antibiotic-producing microorganisms encode many more natural products than previously thought. Biosynthesis of these natural products is tightly regulated by global and cluster situated regulators (CSRs), most of which respond to unknown environmental stimuli, and this likely explains why many biosynthetic gene clusters (BGCs) are not expressed under laboratory conditions. One approach towards novel natural product discovery is to awaken these cryptic BGCs by re-wiring the regulatory control mechanism(s). Most CSRs bind intergenic regions of DNA in their own BGC to control compound biosynthesis, but some CSRs can control the biosynthesis of multiple natural products by binding to several different BGCs. These cross-cluster regulators present an opportunity for natural product discovery, as the expression of multiple BGCs can be affected through the manipulation of a single regulator. This review describes examples of these different mechanisms, including specific examples of cross-cluster regulation, and assesses the impact that this knowledge may have on the discovery of novel natural products.

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Stapp, William B., und Nicholas Polunin. „Global Environmental Education: Towards a Way of Thinking and Acting“. Environmental Conservation 18, Nr. 1 (1991): 13–18. http://dx.doi.org/10.1017/s037689290002124x.

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Our world of Mankind and Nature is becoming more and more seriously threatened as human populations and profligacy increase. Yet short of near-future calamity, there should be hope in global environmental education as a basis for countering such threats as those of world hunger, acidic precipitation, increasing desertification, nuclear proliferation, ‘greenhouse’ warming, and stratospheric ozone depletion. We need to educate people throughout the world to see these dangers in their global context and to act always within this perspective — be they decision-makers, legislators, or mere private citizens. For their actions and effects compound to make up those of their pandominant species, the likes of which our unique planet Earth can surely never have experienced before, and consequently its all-important Biosphere, constituting virtually the whole of our and Nature's lifesupport, is totally unprepared to withstand.The above means that decisions and concomitant actions at the personal level can and often do affect the globe, to however infinitesimal a degree, and of this all people on Earth should be forewarned, acting on it with clear understanding and due responsibility. Particularly North Americans should realize that their effect is disproportionately large, as they use some 36% of the world's resources although comprising only about 6% of its population. Towards remedying such anomalies and effecting an improved sharing of responsibility among all the world's human inhabitants, an urgent need is, clearly, effective global environmental education. We need a world of concerned people with the knowledge that personal decisions and local actions can affect others very widely, and that each individual human being thus has a role in furthering solutions to environmental, as well as political and social problems.With the need for such thinking and action so clear, and the stakes so very high, why is it that global perspectives are not better integrated into today's educational system? ‘The answer is that the barriers to such integration and concomitant action are many and strong, and due understanding of holism's fundamental importance is barely beginning to sweep our prejudice-bound world.’ These barriers include lack of student interest and pertinent enrolment, lack of international perspective among teachers and in the general press, and lack of television and other news-media coverage of such real world affairs. A general obstacle lies in the tendency of educational efforts to emphasize differences rather than similarities — scarcely conducive to fostering an interdependent, one-world ethic. Yet global issues should be our ultimate consideration, and holistic practice our means of furthering them for lasting survival.It is clear that we humans no longer have the option of foregoing a global perspective, and that there is dire need for widely-increased global environmental education to inculcate greatly-increased respect and concern for the world environment. This is brought starkly to mind on realization that practically all the horrors which now beset our world were known fairly widely already twenty years ago — including threats to the stratospheric ozone shield, the ‘greenhouse effect’ on world climate, the effects of deforestation and devegetation with ever-increasing human population pressures, and many more — and that new ones keep on emerging. These latter include build-up of nuclear-waste and other pollutions, AIDS, everincreasing acidic deposition and salinization, flooding of lowlands and other effects of climatic changes, and further foreseeable problems that are likewise of our own making in being due to human overpopulation, ignorance, and/or profligacy.

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Israa N. Witwit, Husham M. Mubark, Hutham Mahmood Yousif Al-Labban und Ahmed Abdul jabbar jaloob Aljanaby. „synthesis and characterization of new imidazole azo ligand with some of transition metal ions, and their biological effect on two pathogenic bacteria of burn patients.“ International Journal of Research in Pharmaceutical Sciences 10, Nr. 3 (12.07.2019). http://dx.doi.org/10.26452/ijrps.v10i3.1382.

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New imidazole azo ligand (DPIDA) was prepared by coupling reaction between 4,5-di phenyl imidazole and N1,N1-dimethylbenzene1,4-diamine di hydrochloride and studied the complexation of this ligand with Mn(II) , Co(II) , Ni(II) , Cu(II) , Zn(II) , Cd(II) , and Hg(II) ions , The free ligand and it’s complexes characterized by Mass, 1HNMR, IR, UV-Vis. , and molar conductivity that indicated the octahedral geometry of them with a bidentate ligand which coordinated from (N3) atom of imidazole ring and one nitrogen atom of azo group.Biological activity of ligand (DPIDA) and it's complexes tested against two multi-drug resistant aerobic pathogenic bacteria isolated from patients with a burn. Three concentrations were selected (50, 100, 150) mg/ml for each crud synthesized derivative compounds. The derivative compound (4,5-diphenyl imidazole) with concentration 150mg/ml had an excellent antibacterial effect against Staphylococcus aureus and Pseudomonas aeruginosa with inhibition zone 21.83 ± 0.1764 mm and 24.30 ± 0.4163 mm respectively.

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Kumar, M. Sathish, und M. Vijey Aanandhi. „Design, Molecular docking, Synthesis and Biological evaluation of 5, 7 dimethyl pyrido(2, 3-d)pyrimidin-4-one and 4,5 dihydro pyrazolo (3, 4-d) pyrimidines for cytotoxic activity“. Research Journal of Pharmacy and Technology, 29.06.2021, 3029–38. http://dx.doi.org/10.52711/0974-360x.2021.00530.

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The fused pyrimidine derivatives are potent tyrosine kinase and thymidylate synthase inhibitors. The compound 3-(4-sulphonyl amino)-2-methyl thio-6-phenyl azo-5, 7-dimethyl pyrido(2,3-d)pyrimidin-4-one was synthesized from Ethyl 2-amino-4,6-dimethylpyridine-3-carboxylate, benzene diazonium chloride, benzene sulphonyl amino isothiocyanate in subsequent reactions. 1-(1, 3-benzothiazol-2-yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidines were synthesized from 1, 3-benzothiazole, 2-thiol, Hydrazine Hydrate, 2-hydrazinyl-1, 3-benzothiazole and aldehydes in subsequent reactions. Twenty-five derivatives pyrimidine scaffolds were designed and performed molecular docking studies for the ability to inhibit the target protein using molecular docking simulation, selective compounds were synthesized and characterized by spectral methods. All the synthesized compounds evaluated for their antioxidant activity and MTT assay exhibited compounds 13c, 13e and 14d can be potential anticancer candidates against MCF-7, Hep G2 and Hela cell lines respectively. Based on all the studies conclude that good agreement was observed between the top-ranked docking scores and top experimental inhibitors when compared with standards ascorbic acid and imatinib. Hence, the compounds could be considered as new anticancer hits for further lead optimization.

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Hassan Abood, Zeid, Zahraa Kadum Chafcheer und Husham Attallah Suhail. „Synthesis and Antibacterial Evaluation of 1,3-Benzoxazepine-1,5-diones bearing Benzothiazole Moiety“. Research Journal of Pharmacy and Technology, 29.04.2021, 1905–9. http://dx.doi.org/10.52711/0974-360x.2021.00336.

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Azo-aldehyde derivative (2) was prepared through reaction of 2-hydroxybenzaldehyde with diazonium ion generated from 2-aminobenzothiazole (1). The producing aldehyde (2) was then treated with some anilines consisting (4-nitroaniline, 3-nitroaniline, 4-aminophenol, 4-methoxyaniline, 4-bromoaniline, 4-chloroaniline and 2,4-dichloroaniline) by (MW) method to give seven Schiff bases (3a-g). Cyloaddition reactions of Schiff bases (3a-g) and phthalic anhydride utilizing (MW) means in dry benzene yielded seven new 1,3-benzoxazepine-1,5-diones (4a-g) carrying the unit of benzothiazole. Determination of verves of final benoxazepines athwart bacteria done on Staphylococcus aurous (Gram-positive) and Escherichia coli (Gram-negative). The outputs showed that all benzoxazepine compounds exhibited greater activity to standard antibiotic (gentamycin) athwart Staphylococcus aurous. Moreover, the benzoxazepines (4a, 4b, 4c, 4d, 4e and 4g) appeared best activity athwart Escherichia coli comparably with that of standard antibiotic.

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Adeleye, Olutayo Ademola, Oluyemisi Adebowale Bamiro, Lateef Gbenga Bakre, Florence Olubola Odeleye, Modupe Nofisat Adebowale, Olufemi Lionel Okunye, Mariam Adeola Sodeinde, Adannaya Charity Adebona und Farid Menaa. „Medicinal Plants with Potential Inhibitory Bioactive Compounds against Coronaviruses“. Advanced Pharmaceutical Bulletin, 30.01.2021. http://dx.doi.org/10.34172/apb.2022.003.

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Medicinal plant is a major source of drug discovery for disease management. Over 85% of the population in Asia and in the Middle East use herbal medicine for disease management such as SARS caused by coronavirus. Infection from coronavirus is initiated by entry of the virus into a susceptible host cell. The two human coronaviruses of public health importance two decades ago were SARS-CoV and MERS-CoV and now SARS-CoV 2. These three viruses belong to the same class of beta coronavirus and are somewhat similar in genome sequencing, life cycle, mode of entry into a host, mode of transmission and clinical manifestations. This review identified twenty medicinal plants with potential inhibitory bioactive compounds from natural sources that are active against coronaviruses that could be developed into various drug delivery systems. It also highlighted several evidences to show that medicinal plant used in the treatment of SARS-CoV may offer some sort of relief from the burden of COVID 19 pandemic. Since there is no specific treatment for COVID 19 yet, the search for medicinal plants with inhibitory bioactive compounds against coronavirus could be the long awaited breakthrough scientists have been searching to change the narratives of Covid-19 pandemic.

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