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Journal articles on the topic 'Were found active against E'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

St. George, Stephanie, Jeanette V. Bishop, Richard G. Titus, and Claude P. Selitrennikoff. "Novel Compounds Active against Leishmania major." Antimicrobial Agents and Chemotherapy 50, no. 2 (2006): 474–79. http://dx.doi.org/10.1128/aac.50.2.474-479.2006.

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ABSTRACT Leishmania major is an important trypanosomatid pathogen that causes leishmaniasis, which is a serious disease in much of the Old World. Current treatments include a small number of antimony compounds that, while somewhat effective, are limited by serious side effects. We have screened a small portion of a unique chemical library and have found at least three novel compounds that are effective against L. tarentolae and L. major in vitro and in a murine macrophage model of L. major infection. These compounds were effective in both assays at doses significantly lower than those of sodiu

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2

Kang, Thierry Roland, Jerome Nyhalah Dinga, Ayuk Elizabeth Orock, Elvis Monya, and Moses Njutain Ngemenya. "Macrofilaricidal Activity, Acute and Biochemical Effects of Three Lichen Species Found on Mount Cameroon." Journal of Parasitology Research 2022 (January 7, 2022): 1–7. http://dx.doi.org/10.1155/2022/1663330.

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Onchocerciasis is a parasitic infection affecting a relatively small population globally but has very devastating pathological outcomes. Ivermectin and recently moxidectin are the only drugs approved for clinical management of the disease, both of which have several limitations. In particular, they are efficacious against microfilariae (microfilaricidal) with no activity against adult worms (nonmacrofilaricidal). Promising anthelmintic activity has been reported in some lichens. This study investigated three lichens, Usnea articulata, Parmotrema tinctorum, and Heterodermia obscurata, found on

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Rajchard, J. " Biologically active substances of bird skin: a review." Veterinární Medicína 55, No. 9 (2010): 413–21. http://dx.doi.org/10.17221/2981-vetmed.

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Bird skin has a number of specific properties. The uropygial gland is a significant skin gland in many species. The secretion of this gland is particularly necessary for maintaining physical characteristics, including feather waterproofing. In some bird species this gland secretion has a repellent effect against potential mammalian predators; in other species it affects the final colour of feathers. In the investigated species of storks (genus Ciconia), secretions of the uropygial gland have been found to be mixtures of monoester waxes, diester waxes, triester waxes and triglycerides. Wax dies

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4

Kumar, Shiv, Nitin Kumar, Sushma Drabu, et al. "Synthesis of 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)acetamide Based Thiazolidinone Derivatives as Potent Antibacterial and Antifungal Agents." E-Journal of Chemistry 9, no. 4 (2012): 2155–65. http://dx.doi.org/10.1155/2012/857514.

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Twelve compounds belonging to series 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-[4-oxo-2-(substituted)phenyl-1,3-thiazolidin-3-yl]acetamide (5a-l) were synthesized. These compounds were evaluated for theirin-vitroantibacterial againstE. coli, S. aureus, K. pneumoniae, P. aeruginosa & antifungalactivity againstC. albicans, A. niger & A. flavusby cup-plate method. Structures of all the newly synthesized compounds were confirmed by elemental analysis,1H-NMR & FT-IR spectral data interpretation. Compounds 5d & 5h having p-nitrophenyl &p-trifluoromethylphenyl group respectively on

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Zeng, Jian, and Zonghan Zhou. "Network Pharmacology-Based Strategy to Reveal the Mechanism of Action of Cistanche Against Cataracts." Current Topics in Nutraceutical Research 21, no. 4 (2023): 454–60. http://dx.doi.org/10.37290/ctnr2641-452x.21:454-460.

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Cistanche is known to relieve cataracts; however, the active ingredients and mechanism of action of cistanche to relieve cataracts are unclear. At present, the active ingredients of cistanche were screened through the Traditional Chinese Medicine Systems Pharmacology website, and a total of six active ingredients were identified. Drug and disease targets were obtained through Swiss target prediction and the Genecard website, and a total of 172 common targets were identified. The biological functions and Kyoto Encyclopedia of Genes and Genomes pathway enrichment of the targets were found to be

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Prajapati, Devang R., Kalpesh V. Vilapara, and Yogesh T. Naliapara. "An Efficient Solid Phase One Port Synthesis of Novel Triazolo[1,5-a]Pyrimidine Derivatives from 4-(4-Aminophenyl)Morpholin-3-One and Evaluation of their Antimicrobial Activity." International Letters of Chemistry, Physics and Astronomy 33 (May 2014): 12–21. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.33.12.

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A series of novel triazolo[1,5-a]pyrimidine derivatives was synthesized from 5-amino-1,2,4-triazole and biologically active morpholinone amine in excellent yield as promising class of antimicrobial agents. The antimicrobial activities were investigated against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogen, Candida albicans, Aspergillusniger, Aspergillusclavatus and compared with standard drugs Ampicillin, Chloramphenicol, Norfloxacin and Griseofulvin. All the synthesized compounds were characterized by IR, 1H NMR, 13C and mass spectroscopy. The result o

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Prajapati, Devang R., Kalpesh V. Vilapara, and Yogesh T. Naliapara. "An Efficient Solid Phase One Port Synthesis of Novel Triazolo[1,5-a]Pyrimidine Derivatives from 4-(4-Aminophenyl)Morpholin-3-One and Evaluation of their Antimicrobial Activity." International Letters of Chemistry, Physics and Astronomy 33 (May 11, 2014): 12–21. http://dx.doi.org/10.56431/p-2k25vg.

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A series of novel triazolo[1,5-a]pyrimidine derivatives was synthesized from 5-amino-1,2,4-triazole and biologically active morpholinone amine in excellent yield as promising class of antimicrobial agents. The antimicrobial activities were investigated against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogen, Candida albicans, Aspergillusniger, Aspergillusclavatus and compared with standard drugs Ampicillin, Chloramphenicol, Norfloxacin and Griseofulvin. All the synthesized compounds were characterized by IR, 1H NMR, 13C and mass spectroscopy. The result o

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8

Luo, Du-Qiang, Xing Zhang, Xuan Tian, and Ji-Kai Liu. "Insecticidal Compounds from Tripterygium wilfordii Active against Mythimna separata." Zeitschrift für Naturforschung C 59, no. 5-6 (2004): 421–26. http://dx.doi.org/10.1515/znc-2004-5-624.

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In the course of our investigations of new sources of higher plant lipids, seed fatty acid compositions and the tocochromanol contents of Salvia bracteata, S. euphratica var. euphratica, S. aucherii var. canascens, S. cryptantha, S. staminea, S. limbata, S. virgata, S. hypargeia, S. halophylla, S. syriaca and S. cilicica were investigated using GLC and HPLC systems. Some of the species are endemic to Turkey. All the Salvia sp. showed the same pattern of fatty acids. Linoleic, linolenic and oleic acid were found as the abundant components. Tocochromanol derivatives of the seed oil showed differ

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9

Heinrich, Michael C., Ajia Town, Marcelina Roberti, Thomas Mühlenberg, and Sebastian Bauer. "In vitro profiling of IDRX-42 against secondary and tertiary mutations (AP/AL) found in TKI-resistant GIST." Journal of Clinical Oncology 43, no. 16_suppl (2025): 11524. https://doi.org/10.1200/jco.2025.43.16_suppl.11524.

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11524 Background: The majority of Gastrointestinal Stromal Tumors (GIST) harbor a KIT mutation and respond to imatinib (IM), but over time clinical resistance emerges due to secondary mutations. These secondary mutations are restricted to two regions of the KIT protein: the drug/ATP binding pocket (AP, exons 13 and 14) and the activation loop (AL, exons 17 and 18). Although additional TKI drugs has been approved for later lines of therapy, these agents lack activity against the entire spectrum of known secondary resistance mutations. For example, sunitinib is potent against AP mutations (V654A

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Ali, Asad, Ram Kumar, Jana Mazákova, Marie Maňasová, Miloslav Zouhar, and Matěj Pánek. "Evaluation of the Ability of Seven Active Ingredients of Fungicides to Suppress Phytophthora cactorum at Diverse Life Stages, and Variability in Resistance Found among Isolates." Journal of Fungi 8, no. 10 (2022): 1039. http://dx.doi.org/10.3390/jof8101039.

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Phytophthora cactorum is considered an important plant pathogen which is causing major damage to strawberry plants worldwide. In the current study, the ability of the active ingredients of seven different fungicides, azoxystrobin, cymoxanil, dimethomorph, fenamidone, fluopicolide, metalaxyl and propamocarb, to suppress the mycelial growth, sporangial formation and zoospore release of P. cactorum isolates, was tested. The variation in resistance against various fungicides was found among the isolates. The active ingredients are also unequally efficient against different life stages of P. cactor

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Ellsworth, Katelyn T., Trevor N. Clark, Christopher A. Gray, and John A. Johnson. "Isolation and bioassay screening of medicinal plant endophytes from eastern Canada." Canadian Journal of Microbiology 59, no. 11 (2013): 761–65. http://dx.doi.org/10.1139/cjm-2013-0639.

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Eighty-one distinct fungal endophytes were isolated from 12 traditionally used medicinal plants from New Brunswick, Canada. This is the first report of endophytes from 8 of the 12 host plants. One hundred and sixty-two crude extracts derived from the mycelia and spent fermentation broths of liquid cultures of each endophyte were screened for antibacterial and antifungal activity. Twenty-two extracts were active against Staphylococcus aureus while 30 were active against Pseudomonas aeruginosa. Twelve crude extracts were found to be active against Candida albicans.

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12

N, Liliwirianis, Wan Zuraida Wan Mohd Zain, Jamaluddin Kassim, and Shaikh Abdul Karim. "Antimicrobial Activity of Plant Extracts againstBacillus Subtilis,Staphylococcus Aureusand Escherichia Coli." E-Journal of Chemistry 8, s1 (2011): S282—S284. http://dx.doi.org/10.1155/2011/824697.

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Local herbs have many potential that may be active with antimicrobial activity. A screening was conducted with 11 species of herbs collected in UiTM Pahang Forest Reserve.Epipremnumsp.,Zingibersp.Tetracera indica, Tectaria crenata, Piper stylosum, Homalomena propinque, Goniothalamus sp., Elephantopus scaber, Mapania patiolale, Melastomasp.,Stemona tuberosa, Phullagathis rotundifolia, Thotea grandifoliaandSmilaxsp. were extracted with methanol to obtain their crude. The agar diffusion method using blank disc of 6 mm diameter were loaded with 1000 µg/mL of methanol crude and applied to the inocu

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Sharma, Puja, Rajat Patel, Rohit R. Koshti, Akshay Vyas, and Chetan B. Sangani. "Synthesis, Characterization, Biological Evaluation, DFT Studies and Molecular Docking of Novel 12-(2-(1H-Imidazol-1-yl)quinolin-3-yl)-8-methyl-2,3,4,12-tetrahydro- 1H-benzo[4,5]thiazolo[2,3-b]quinazolin-1-one and its Derivatives." Asian Journal of Chemistry 35, no. 9 (2023): 2092–102. http://dx.doi.org/10.14233/ajchem.2023.28081.

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Twelve new compounds were synthesized consisting of biquinoline-imidazole-benzothiazole hybrids 6a-l using a base catalyzed one pot MCR reaction, these were then screened for in vitro biological activities against cancer cell lines. Among the twelve prepared potential anticancer agents, compound 6j was found to be the most active against EGFR (IC50 of 0.14 ± 0.03 Μm), A549 and HepG2, also the same derivative of the series was found to be most active against FabH (IC50 of 3.1 Μm) E. coli. Further the molecules were analysed for DFT and molecular docking studies to calculate the distance and ang

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14

Pereira, Juliana Vianna, Débora Cristina Baldoqui Bergamo, José Odair Pereira, Suzelei de Castro França, Rosemeire Cristina Linhares Rodrigues Pietro, and Yara T. Corrêa Silva-Sousa. "Antimicrobial activity of Arctium lappa constituents against microorganisms commonly found in endodontic infections." Brazilian Dental Journal 16, no. 3 (2005): 192–96. http://dx.doi.org/10.1590/s0103-64402005000300004.

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This study evaluated in vitro the antimicrobial activity of rough extracts from leaves of Arctium lappa and their phases. The following microorganisms, commonly found in the oral cavity, specifically in endodontic infections, were used: Enterococcus faecalis, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis and Candida albicans. The agar-diffusion method allowed detection of the hexanic phase as an inhibitor of microbial growth. Bioautographic assays identified antimicrobial substances in the extract. The results showed the existence, in the rough hexanic phase and in its fract

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15

Desai, Nisheeth C., and Tushar J. Karkar. "Synthesis and Characterization of Some Novel Coumarin Based 2-Pyridone Heterocycles with their Broad Spectrum Antimicrobial Potency." International Letters of Chemistry, Physics and Astronomy 66 (May 2016): 1–12. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.66.1.

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The synthesis of a novel series of 6-((arylidene) amino)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl) ethylidene) amino)-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o were synthesized and structures of compounds have been elucidated by IR,1H NMR,13C NMR and mass spectral data. Antimicrobial activity was measured against certain strains of bacteria and fungi by serial broth dilution. Evaluation of antimicrobial activity shown that the compounds (4g, 4j, 4k and 4o) were found to be most active against selected bacterial strains and compounds (4d, 4m and 4n) were found to be most active against se

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16

Desai, Nisheeth C., and Tushar J. Karkar. "Synthesis and Characterization of Some Novel Coumarin Based 2-Pyridone Heterocycles with their Broad Spectrum Antimicrobial Potency." International Letters of Chemistry, Physics and Astronomy 66 (May 30, 2016): 1–12. http://dx.doi.org/10.56431/p-5vyfc4.

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The synthesis of a novel series of 6-((arylidene) amino)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl) ethylidene) amino)-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o were synthesized and structures of compounds have been elucidated by IR, 1H NMR, 13C NMR and mass spectral data. Antimicrobial activity was measured against certain strains of bacteria and fungi by serial broth dilution. Evaluation of antimicrobial activity shown that the compounds (4g, 4j, 4k and 4o) were found to be most active against selected bacterial strains and compounds (4d, 4m and 4n) were found to be most active against

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17

Pohlit, Adrian Martin, Etienne Louis Jacques Quinard, Sergio Massayoshi Nunomura, et al. "Screening of plants found in the State of Amazonas, Brazil for activity against Aedes aegypti larvae." Acta Amazonica 34, no. 1 (2004): 97–105. http://dx.doi.org/10.1590/s0044-59672004000100012.

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Ethanol, methanol and water extracts representing mostly native plant species found in the Amazon region were prepared, respectively, by maceration, continuous liquid-solid extraction and infusion, followed by evaporation and freeze-drying. The freeze-dried extracts were tested for lethality toward Aedes aegypti larvae at test concentrations of 500 mg / mL. In general, methanol extracts exhibited the greatest larvicidal activity. The following 7 methanol extracts of (the parts of) the indicated plant species were the most active, resulting in 100% mortality in A. aegypti larvae: Tapura amazoni

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18

Feldmann, Christian, Filip Miljković, Dimitar Yonchev, and Jürgen Bajorath. "Identifying Promiscuous Compounds with Activity against Different Target Classes." Molecules 24, no. 22 (2019): 4185. http://dx.doi.org/10.3390/molecules24224185.

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Compounds with multitarget activity are of high interest for polypharmacological drug discovery. Such promiscuous compounds might be active against closely related target proteins from the same family or against distantly related or unrelated targets. Compounds with activity against distinct targets are not only of interest for polypharmacology but also to better understand how small molecules might form specific interactions in different binding site environments. We have aimed to identify compounds with activity against drug targets from different classes. To these ends, a systematic analysi

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19

Pérez, Cristina, and Claudia Anesini. "Antibacterial Activity of Alimentary Plants Against Staphylococcus aureus Growth." American Journal of Chinese Medicine 22, no. 02 (1994): 169–74. http://dx.doi.org/10.1142/s0192415x94000206.

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Alimentary plants were screened for antibacterial activity against a penicillin G resistant strain of Staphylococcus aureus. Twenty-five samples of plant material corresponding to 21 species from 13 families were used. Both aqueous and ethanol extracts were obtained from them. Antibacterial activity was determined by the agar-well diffusion method, using cephazolin as a standard antibiotic. Seventeen ethanol extracts were found active. Eugenia caryophyllata (clavo de olor*) flowers, Myristica fragans (nuez moscada*) seeds, Theobroma cacao (cacao*) seed bark, Triticum sp (trigo*) fruit, Zea may

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20

Shaikh, Mubarak H., Dnyaneshwar D. Subhedar, Laxman Nawale, et al. "Novel Benzylidenehydrazide-1,2,3-Triazole Conjugates as Antitubercular Agents: Synthesis and Molecular Docking." Mini-Reviews in Medicinal Chemistry 19, no. 14 (2019): 1178–94. http://dx.doi.org/10.2174/1389557518666180718124858.

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Background & Objectives:Novel 1,2,3-triazole based benzylidenehydrazide derivatives were synthesized and evaluated for antitubercular activity against Mycobacterium tuberculosis (MTB) H37Ra, M. bovis BCG and cytotoxic activity. Most of the derivatives exhibited promising in vitro potency against MTB characterized by lower MIC values.Methods:Among all the synthesized derivatives, compound 6a and 6j were the most active against active and dormant MTB H37Ra, respectively. Compound 6d was significantly active against dormant and active M. bovis BCG.Results:The structure activity relationship h

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SONAL, SHAH, and H. MEHTA R. "Synthesis of some New 8-Methoxy-5-substituted-amino- methylcoumarins as Possible Antibacterial Agents." Journal of Indian Chemical Society Vol.66, Nov 1997 (1989): 802–3. https://doi.org/10.5281/zenodo.5996422.

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Department of Chemistry, Faculty of Science, M. S. University of Baroda, Baroda-390 002 <em>Manuscript received 27 February 1989, revised 21 June 1989, accepted 26 June 1989</em> <strong>A number of 8-methoxy-5-substituted-coumarins have been synthesised by chloromethylation of 8-methoxycoumarin and subsequent condensation of the chloromethyl compound with ultimo amines. Their structures were established by analytical data and spectral studies. Some of the compounds were found active against <em>E. coli, </em>and <em>S. aureus</em></strong>

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Mandell, Gerald L., and Elizabeth J. Coleman. "Activities of Antimicrobial Agents against Intracellular Pneumococci." Antimicrobial Agents and Chemotherapy 44, no. 9 (2000): 2561–63. http://dx.doi.org/10.1128/aac.44.9.2561-2563.2000.

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ABSTRACT Pneumococci can enter and survive inside human lung alveolar carcinoma cells. We examined the activity of azithromycin, gentamicin, levofloxacin, moxifloxacin, penicillin G, rifampin, telithromycin, and trovafloxacin against pneumococci inside and outside cells. We found that moxifloxacin, trovafloxacin, and telithromycin were the most active, but only telithromycin killed all intracellular organisms.

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Abedini, Amin, Vincent Roumy, Séverine Mahieux, et al. "Rosmarinic Acid and Its Methyl Ester as Antimicrobial Components of the Hydromethanolic Extract ofHyptis atrorubensPoit. (Lamiaceae)." Evidence-Based Complementary and Alternative Medicine 2013 (2013): 1–11. http://dx.doi.org/10.1155/2013/604536.

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Primary biological examination of four extracts of the leaves and stems ofHyptis atrorubensPoit. (Lamiaceae), a plant species used as an antimicrobial agent in Guadeloupe, allowed us to select the hydromethanolic extract of the stems for further studies. It was tested against 46 microorganismsin vitro. It was active against 29 microorganisms. The best antibacterial activity was found against bacteria, mostly Gram-positive ones. Bioautography enabled the isolation and identification of four antibacterial compounds from this plant: rosmarinic acid, methyl rosmarinate, isoquercetin, and hyperosid

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Chen, Xiao Hui, Chul-Sa Kim, Takehiro Kashiwagi, Shin-ich Tebayashi, and Michio Horiike. "Antifeedants against Acusta despesta from the Japanese Cedar, Cryptomeria japonica." Zeitschrift für Naturforschung C 56, no. 3-4 (2001): 249–52. http://dx.doi.org/10.1515/znc-2001-3-413.

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Abstract During our studies on the components in Japanese cedar, Cryptomeria japonica, we found that the crude methanol extract of C. japonica showed intense antifeeding activity against one snail species, Acusta despesta, which is well-known as a pest of many vegetables and crops. The active components in the extract were separated into the hexane and ethyl acetate soluble fractions. From the active ethyl acetate soluble fraction, two norlignans, sequirin-C and agatharesinol, were isolated and identified as the active compounds. Both compounds inhibited feeding behavior of A. despesta at 30 μ

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Mancuso, Monique, and Renata Zaccone. "Citrus Essential Oils’ Antibacterial Effects against Food-Borne Bacteria." Recent Advances in Biology and Medicine 6, no. 3 (2020): 1–3. http://dx.doi.org/10.18639/rabm.2020.9800003.

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Seven citrus essential oils (CEOs) and fourterpenes were tested againstelevenbacterial pathogenic strains isolated from food to evaluate the antimicrobial effects. All CEOs presented antibacterial activities. In particular, CEOs were very active against StaphylococcusEpidermidis, which was found to be the most sensitive toward all oils, showing high growth inhibition.

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Erazo, Silvia, Giovanna Rocco, Mercedes Zaldivar, et al. "Active Metabolites from Dunalia spinosa Resinous Exudates." Zeitschrift für Naturforschung C 63, no. 7-8 (2008): 492–96. http://dx.doi.org/10.1515/znc-2008-7-804.

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Dunalia spinosa, a plant used in folk medicine for toothaches, breathing problems and cleansing wounds, was found active as antimicrobial and antioxidant. A new (E)-aurone rutinoside (dunaurone) has been isolated from the aerial parts of the plant, and its structure was determined by spectroscopic means. Lupeol, ß-sitosterol, scopoletin, quercetin and withaferin A were also found. All the extracts exhibited strong antimicrobial activity while dunaurone showed only weak antimicrobial inhibition against Klebsiella pneumoniae; in addition it presented a significant free radical scavenging activit

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Hochma, Efrat, Iryna Hovor, Faina Nakonechny, and Marina Nisnevitch. "Photo- and Sono-Active Food Colorants Inactivating Bacteria." International Journal of Molecular Sciences 24, no. 20 (2023): 15126. http://dx.doi.org/10.3390/ijms242015126.

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Food colorants are commonly used as excipients in pharmaceutical and nutraceutical fields, but they have a wide range of other potential applications, for instance, as cytotoxic drugs or mediators of physical antimicrobial treatments. The photodynamic antibacterial activity of several edible food colorants is reported here, including E127, E129, E124, E122, E133, and E150a, alongside Rhein, a natural lipophilic antibacterial and anticancer compound found in medicinal plants. Minimal inhibitory concentration (MIC) values for S. aureus and E. coli showed that E127 and Rhein were effective agains

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Patel, Rajat, Puja Sharma, Rohit R. Koshti, Akshay Vyas, and Chetan B. Sangani. "Synthesis, Biological Evaluation, DFT Studies and Molecular Docking of Novel 4-(5-(1H-Imidazol-1-yl)-3-methyl-1-phenyl-1H-pyrazol-4-yl)-6-amino-3-methyl- 1-phenyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile and its Derivatives." Asian Journal of Chemistry 35, no. 7 (2023): 1616–24. http://dx.doi.org/10.14233/ajchem.2023.27921.

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A novel series consisting of eight imidazol-pyrazole hybrids ( 9a-h) are synthesized using a base catalyzed one pot multi-component reaction (MCR) and screened for in vitro biological activities. All compounds were found to display high biological activities but compound 9g was found to be the most active against EGFR (IC50 of 0.11 ± 0.02 μm), A549 and HepG2, while compound 9h was found to be most active against FabH (IC50 of 2.6 μm) E. coli. The DFT studies and molecular docking was done for compounds 9a-h to calculate the distance and angle between the active parts of the molecules and charg

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Bakuradze, Nata, Maia Merabishvili, Ia Kusradze, et al. "Characterization of a Bacteriophage GEC_vB_Bfr_UZM3 Active against Bacteroides fragilis." Viruses 15, no. 5 (2023): 1042. http://dx.doi.org/10.3390/v15051042.

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Bacteroides fragilis is a commensal gut bacterium that is associated with a number of blood and tissue infections. It has not yet been recognized as one of the drug-resistant human pathogens, but cases of the refractory infections, caused by strains that are not susceptible to the common antibiotic regimes established for B. fragilis, have been more frequently reported. Bacteriophages (phages) were found to be a successful antibacterial alternative to antibiotic therapy in many cases of multidrug-resistant (MDR) bacterial infections. We have characterized the bacteriophage GEC_vB_Bfr_UZM3 (UZM

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Vale-Costa, Sílvia, Nuno Vale, Joana Matos, et al. "Peptidomimetic and Organometallic Derivatives of Primaquine Active against Leishmania infantum." Antimicrobial Agents and Chemotherapy 56, no. 11 (2012): 5774–81. http://dx.doi.org/10.1128/aac.00873-12.

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ABSTRACTThe current treatment of visceral leishmaniasis is made difficult by the low efficacy, elevated costs, low bioavailability, and high toxicity of many of the available drugs. Primaquine, an antimalarial 8-aminoquinoline, displays activity againstLeishmaniaspp., and several of its derivatives have been developed as potential antileishmanial drugs. However, primaquine exhibits low oral bioavailability due to oxidative deamination of its aliphatic chain. We previously developed peptidomimetic and organometallic derivatives of primaquine, with higher resistance to proteolytic degradation an

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Osmolovsky, A. A., A. A. Shestakova, D. Ye Surkova, R. Lehotská, and E. Piecková. "INVESTIGATION OF NEW ASPERGILLUS STRAINS AS PRODUCERS OF HEMOSTATICALLY ACTIVE PROTEASES." Vestnik Moskovskogo universiteta. Seria 16. Biologia 78, no. 2, 2023 (2023): 109–14. http://dx.doi.org/10.55959/msu0137-0952-16-78-2-7.

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For ve species of Aspergillus micromycetes, the diversity of proteolytic activities against human hemostasis proteins was assessed. For every strain, absence of activities similar to hemostatic proteases - thrombin, plasmin, factor Xa, urokinase, and protein C was shown. In addition, no activating activities towards precursors of the named proteases were demonstrated. For A. glaucus, proteases of high activity (58,52 Utyr) and speci city against brinogen were found. A. athecius, A. caespitosus и A. wentii, were capable of proteolysis at acidic pH.

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Agbo, Gildenhuys та Mphahlele. "Inhibitory Effects of Novel 7-Substituted 6-iodo-3-O-Flavonol Glycosides against Cholinesterases and β-secretase Activities, and Evaluation for Potential Antioxidant Properties". Molecules 24, № 19 (2019): 3500. http://dx.doi.org/10.3390/molecules24193500.

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A series of 7-halogeno- (X = F, Cl, Br) and 7-methoxy-substituted acetylated 6-iodo-3-O-flavonol glycosides were prepared, and evaluated for inhibitory effect in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. 7-Bromo-2-(4-chlorophenyl)-6-iodo-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-β-d-glucopyranoside (2k) and 7-bromo-6-iodo-2-(4-methoxyphenyl)-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-β-d-glucopyranoside (2l) exhibited significant inhibitory effect against AChE activity when compared to the activity of the reference standard, donepezil. Compound 2k

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Samaraweera, Thumuli, Thummini Samaraweera, Nimesha Senadeera, and Chathuranga B. Ranaweera. "Evaluation of Antibacterial Activity of Endemic Jeffreycia zeylanica Plant Found in Sri Lanka." South Asian Journal of Research in Microbiology 16, no. 1 (2023): 1–9. http://dx.doi.org/10.9734/sajrm/2023/v16i1296.

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Aims: Determination of antibacterial efficacy of aqueous, methanol, dichloromethane, and hexane extracts from Jeffreycia zeylanica leaves against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. Methodology: Completely ballooned leaves of J. zeylanica were gathered, air-dried, and milled into fine powder. Then macerated in all four selected solvents for about 1-2 weeks, the extracts were obtained by vacuum evaporation under reduced pressure. Antibacterial activity was performed against Staphylococcus aureus (ATCC25923), Escherichia coli (ATCC 25922), and Pseudomonas a

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Różycka, Daria, Małgorzata Korycka-Machała, Anna Żaczek, et al. "Novel Isoniazid-Carborane Hybrids Active In Vitro against Mycobacterium tuberculosis." Pharmaceuticals 13, no. 12 (2020): 465. http://dx.doi.org/10.3390/ph13120465.

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Tuberculosis (TB) is a severe infectious disease with high mortality and morbidity. The emergence of drug-resistant TB has increased the challenge to eliminate this disease. Isoniazid (INH) remains the key and effective component in the therapeutic regimen recommended by World Health Organization (WHO). A series of isoniazid-carborane derivatives containing 1,2-dicarba-closo-dodecaborane, 1,7-dicarba-closo-dodecaborane, 1,12-dicarba-closo-dodecaborane, or 7,8-dicarba-nido-undecaborate anion were synthesized for the first time. The compounds were tested in vitro against the Mycobacterium tuberc

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Hacioglu, Mayram, Ayse Seher Birteksoz Tan, Sibel Dosler, Nese Inan, and Gulten Otuk. "In vitroactivities of antifungals alone and in combination with tigecycline againstCandida albicansbiofilms." PeerJ 6 (July 25, 2018): e5263. http://dx.doi.org/10.7717/peerj.5263.

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BackgroundCandidamay form biofilms, which are thought to underlie the most recalcitrant infections.MethodsIn this study, activities of antifungal agents alone and in combination with tigecycline against planktonic cells and mature and developing biofilms ofCandida albicansisolates were evaluated.ResultsAmphotericin B and echinocandins were found to be the most effective agents against mature biofilms, whereas the least effective agent was fluconazole. Furthermore, the most effective anti-fungal monotherapies against biofilm formation were amphotericin B and anidulafungin, and the least effecti

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Mozhaitsev, Evgenii S., Alexandra L. Zakharenko, Evgeniy V. Suslov, et al. "Novel Inhibitors of DNA Repair Enzyme TDP1 Combining Monoterpenoid and Adamantane Fragments." Anti-Cancer Agents in Medicinal Chemistry 19, no. 4 (2019): 463–72. http://dx.doi.org/10.2174/1871520619666181207094243.

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Background and Objective: The DNA repair enzyme tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a current inhibition target to improve the efficacy of cancer chemotherapy. Previous studies showed that compounds combining adamantane and monoterpenoid fragments are active against TDP1 enzyme. This investigation is focused on the synthesis of monoterpenoid derived esters of 1-adamantane carboxylic acid as TDP1 inhibitors. Methods: New esters were synthesized by the interaction between 1-adamantane carboxylic acid chloride and monoterpenoid alcohols. The esters were tested against TDP1 and its binding t

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Mason, R. W. "Characterization of the active site of human multicatalytic proteinase." Biochemical Journal 265, no. 2 (1990): 479–84. http://dx.doi.org/10.1042/bj2650479.

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The activity of multicatalytic proteinase against synthetic substrates and the kinetics of its inhibition by a range of class-specific inhibitors have been investigated. The enzyme was found to have a broader pH activity profile than previously noted, being active against succinyl-Ala-Ala-Phe-7-amino-4-methylcoumarin optimally at pH 4.5 and against benzyloxycarbonyl-Gly-Gly-Arg-7-amino-4-methylcoumarin optimally at pH 10.5. Neither activity was inhibited by the class-specific inhibitors 1,10-phenanthroline, EDTA, pepstatin, di-isopropyl fluorophosphate, peptidyl chloromethanes, peptidyl diazom

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T G, Shruthi, Sangeetha Subramanian, and Sumesh Eswaran. "Design, Synthesis and Study of Antibacterial and Antitubercular Activity of Quinoline Hydrazone Hybrids." Heterocyclic Communications 26, no. 1 (2020): 137–47. http://dx.doi.org/10.1515/hc-2020-0109.

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AbstractEmerging bacterial resistance is causing widespread problems for the treatment of various infections. Therefore, the search for antimicrobials is a never-ending task. Hydrazones and quinolines possess a wide variety of biological activities. Herewith, eleven quinoline hydrazone derivatives have been designed, synthesized, characterized and evaluated for their antibacterial activity and antitubercular potential against Mtb WT H37Rv. Compounds QH-02, QH-04 and QH-05 were found to be promising compounds with an MIC value of 4 μg/mL against Mtb WT H37Rv. Compounds QH-02, QH-04, QH-05, and

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Syarifah, Syarifah, Elfita Elfita, Hary Widjajanti, Arum Setiawan, and Alfia Rahma Kurniawati. "Active Compound Phenyl Ether from Potential Endophytic Fungi of Syzygium zeylanicum." Trends in Sciences 20, no. 9 (2023): 5480. http://dx.doi.org/10.48048/tis.2023.5480.

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Endophytic fungi can be found in various types of plants, especially medicinal plants, such as Syzygium zeylanicum, one of the many medicinal plants found in Indonesia. This study aimed to obtain isolates of endophytic fungi from the bark of Syzygium zeylanicum, L., with antibacterial and antioxidant activities and identify their bioactive compounds. Characterization of endophytic fungi was carried out morphologically and fungi that showed high bioactivity were characterized molecularly. Antibacterial activity was carried out by disc diffusion method and antioxidant activity by DPPH method. Is

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Torres, Ana M., Francisco J. Camargo, Gabriela A. L. Ricciardi, Armando I. A. Ricciardi, and Eduardo Dellacassa. "Neutralizing Effects of Nectandra angustifolia Extracts against Bothrops neuwiedi Snake Venom." Natural Product Communications 6, no. 9 (2011): 1934578X1100600. http://dx.doi.org/10.1177/1934578x1100600942.

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Leaves extracts and essential oil of Nectandra angustifolia were explored for the first time for neutralization of Bothrops neuwiedi diporus snake venom. The ethanol extract was the most active and inhibited both venom activities (hemolytic and coagulant), while the oil was only active on the coagulant activity. These observations confirmed that certain medicinal plants from Corrientes and Chaco Provinces possess significant snake venom neutralizing capacity and need further examination for their active constituents. Analysis by GC and GC-MS of the essential oil and the enantiomeric excess fou

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Ryan, Lisa K., Katie B. Freeman, Jorge A. Masso-Silva, et al. "Activity of Potent and Selective Host Defense Peptide Mimetics in Mouse Models of Oral Candidiasis." Antimicrobial Agents and Chemotherapy 58, no. 7 (2014): 3820–27. http://dx.doi.org/10.1128/aac.02649-13.

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ABSTRACTThere is a strong need for new broadly active antifungal agents for the treatment of oral candidiasis that not only are active against many species ofCandida, including drug-resistant strains, but also evade microbial countermeasures which may lead to resistance. Host defense peptides (HDPs) can provide a foundation for the development of such agents. Toward this end, we have developed fully synthetic, small-molecule, nonpeptide mimetics of the HDPs that improve safety and other pharmaceutical properties. Here we describe the identification of several HDP mimetics that are broadly acti

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FRIEDMAN, MENDEL, PHILIP R. HENIKA, and ROBERT E. MANDRELL. "Antibacterial Activities of Phenolic Benzaldehydes and Benzoic Acids against Campylobacter jejuni, Escherichia coli, Listeria monocytogenes, and Salmonella enterica." Journal of Food Protection 66, no. 10 (2003): 1811–21. http://dx.doi.org/10.4315/0362-028x-66.10.1811.

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We evaluated the bactericidal activities of 35 benzaldehydes, 34 benzoic acids, and 1 benzoic acid methyl ester against Campylobacter jejuni, Escherichia coli O157:H7, Listeria monocytogenes, and Salmonella enterica when these compounds were substituted on the benzene ring with 0, 1, 2, or 3 hydroxy (OH) and/or methoxy (OCH3) groups in a pH 7.0 buffer. Dose-response plots were used to determine the percentage of the sample that induced a 50% decrease in CFU after 60 min (BA50). Of the 70 compounds tested, 24 were found to be active against all four pathogens, and additional 4, 10, and 12 were

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Veiga, Andreza do Socorro Silva da, Heliton Patrick Cordovil Brígido, Sandro Percário, Andrey Moacir do Rosário Marinho, and Maria Fâni Dolabela. "Antileishmanial potential of alkaloids isolated from plants: an integrative review." Research, Society and Development 9, no. 10 (2020): e9119109334. http://dx.doi.org/10.33448/rsd-v9i10.9334.

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Leishmaniasis treatment is often carried out with drugs of high toxic potential and high cost, and satisfactory therapeutic response is not usually observed. In this context, searching for therapeutic alternatives is urgent. This study seeks to evaluate the antileishmanial potential of alkaloids from plants. The search for scientific papers occurred at Pubmed, CAPES Journal Portal (PPC), Virtual Health Library (VHL) and COCHRANE using the descriptors: alkaloid and antileishmanial. The inclusion criteria were studies about alkaloids isolated from plants and tested against Leishmania parasite. A

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Venegas-Casanova, E. A., R. D. D. G. de Albuquerque, F. T. Cerna-Reyes, G. K. Céspedes-Cáceres, F. R. Rubio López, and S. L. Rodríguez-Chamorro. "Comprehensive Review: Essential Oils found in Africa and Asia as Green Controllers of <em>Bemisia tabaci</em>, a Worldwide Agronomical Pest." Journal of Agricultural Sciences – Sri Lanka 19, no. 3 (2024): 548–65. http://dx.doi.org/10.4038/jas.v19i3.10325.

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Purpose: Agricultural losses caused by pests have a profound impact on African and Asian countries. In this context, the whitefly Bemisia tabaci is an important global pest and attacks many vegetables. However, conventional pesticides cause unwanted effects on the environment and consumers, in addition to the development of resistance. Therefore, sustainable resources have been used and researched, including thoseof natural origin.Research Method: The objective of this review was to compile and discuss studies of essential oils found in Asian and African countries with action against B. tabaci

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45

Cuenca-Estrella, Manuel, Alicia Gomez-Lopez, Emilia Mellado, Maria J. Buitrago, Araceli Monzon, and Juan Luis Rodriguez-Tudela. "Head-to-Head Comparison of the Activities of Currently Available Antifungal Agents against 3,378 Spanish Clinical Isolates of Yeasts and Filamentous Fungi." Antimicrobial Agents and Chemotherapy 50, no. 3 (2006): 917–21. http://dx.doi.org/10.1128/aac.50.3.917-921.2006.

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ABSTRACT We have compared the activities of posaconazole and other currently available antifungal agents against a collection of 3,378 clinical isolates of yeasts and filamentous fungi. A total of 1,997 clinical isolates of Candida spp., 359 of other yeast species, 697 strains of Aspergillus spp., and 325 nondermatophyte non-Aspergillus spp. were included. The average geometric means of the MICs of agents that were tested against Candida spp. were 0.23 μg/ml for amphotericin B, 0.29 μg/ml for flucytosine, 0.97 μg/ml for fluconazole, 0.07 μg/ml for itraconazole, 0.04 μg/ml for voriconazole, 0.1

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Duddu, Midhun Kumar, and Girijasankar Guntuku. "ISOLATION, SCREENING AND CHARACTERIZATION OF ANTIBIOTIC PRODUCING ACTINOMYCETES FROM KAPULUPPADA PLASTIC WASTE DUMPING YARD, VISAKHAPATNAM." International Journal of Pharmacy and Pharmaceutical Sciences 8, no. 11 (2016): 221. http://dx.doi.org/10.22159/ijpps.2016v8i11.10110.

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Objective: To isolate, screen and characterize antibiotic producing actinomycetes from Kapuluppada plastic waste dumping yard, Visakhapatnam.Methods: A total of 12 soil samples were collected, serially diluted and spread on starch casein agar supplemented with Rifampicin and Cycloheximide for inhibition of bacteria and fungi, respectively. Cross-streak method was used to check the antagonistic activity of isolated actinomycetes against bacteria and fungi. Crude extracts from submerged state fermentation were used for the production of antimicrobial compounds. Agar well diffusion method was use

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Jørgensen, Karin Meinike, Marie Helleberg, Rasmus Krøger Hare, Lise Nistrup Jørgensen, and Maiken Cavling Arendrup. "Dissection of the Activity of Agricultural Fungicides against Clinical Aspergillus Isolates with and without Environmentally and Medically Induced Azole Resistance." Journal of Fungi 7, no. 3 (2021): 205. http://dx.doi.org/10.3390/jof7030205.

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Azole resistance is an emerging problem in patients with aspergillosis. The role of fungicides for resistance development and occurrence is not fully elucidated. EUCAST reference MICs of 17 fungicides (11 azoles and 6 others), five azole fungicide metabolites and four medical triazoles were examined against two reference and 28 clinical isolates of A. fumigatus, A. flavus and A. terreus with (n = 12) and without (n = 16) resistance mutations. Eight/11 azole fungicides were active against wild-type A. fumigatus, A. flavus and A. terreus, including four (metconazole, prothioconazole-desthio, pro

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Abdul Qadir, Muhammad, Mahmood Ahmed, Hina Aslam, Sadia Waseem, and Muhammad Imtiaz Shafiq. "Amidine Sulfonamides and Benzene Sulfonamides: Synthesis and Their Biological Evaluation." Journal of Chemistry 2015 (2015): 1–8. http://dx.doi.org/10.1155/2015/524056.

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New amidine and benzene sulfonamide derivatives were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS,1HNMR, and13CNMR). In vitro, developed compounds were screened for their antibacterial and antifungal activities against medically important bacterial strains, namely,S. aureus, B. subtilis, andE. coli, and fungi, namely,A. flavus, A. parasiticus, andA.sp. The antibacterial and antifungal activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compoun

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Daunes, Sylvie, and Claudius D'Silva. "Glutathione Derivatives Active against Trypanosoma brucei rhodesiense and T.brucei brucei In Vitro." Antimicrobial Agents and Chemotherapy 46, no. 2 (2002): 434–37. http://dx.doi.org/10.1128/aac.46.2.434-437.2002.

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ABSTRACT Diesters based on N-benzyloxycarbonyl-S-(2,4-dinitrophenyl) GSH (CBzGSDNP) containing linear alcohols 3 to 9, branched alcohols 10 to 20, or heteroatom linear alcohols 21 to 25, were investigated as in vitro inhibitors of pathogenic parasites. Diesters 3 to 25 were better inhibitors of Trypanosoma brucei rhodesiense than of T. brucei brucei and had low cytotoxicities. The most active compound had a 50% effective dose (ED50) of 0.2 μM. A quantitative structure activity regression equation relating the log (1/ED50) versus the hydrophobicity parameter (log P), Taft's steric parameter (Es

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Soares, Deivid C., Nathalya A. Portella, Mônica Freiman de S. Ramos, Antonio C. Siani та Elvira M. Saraiva. "Trans-β-Caryophyllene: An Effective Antileishmanial Compound Found in Commercial Copaiba Oil (Copaiferaspp.)". Evidence-Based Complementary and Alternative Medicine 2013 (2013): 1–13. http://dx.doi.org/10.1155/2013/761323.

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This study investigated the leishmanicidal activity againstLeishmania amazonensisof four commercial oils fromCopaiferaspp. named as C1, C2, C3, and C4, the sesquiterpene and diterpene pools obtained from distilling C4, and isolatedβ-caryophyllene (CAR). Copaiba oils chemical compositions were analyzed by gas chromatography and correlated with biological activities. Diterpenes-rich oils C2 and C3 showed antipromastigote activity. Sesquiterpenes-rich C1 and C4, and isolated CAR presented a dose-dependent activity against intracellular amastigotes, with IC50sof 2.9 µg/mL, 2.3 µg/mL, and 1.3 µg/mL

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