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Simple method for preparation of Dialkyl (2,3-dihydro-1,3-thiazol-2-yl)-phosphonates
PublicationAbstract A simple synthesis of dialkyl (2,3-dihydro-1,3-thiazol-2-yl)-phosphonates from thiazoliumsalts and trialkyl phosphites is described. The series of dialkyl (2,3-dihydro-1,3-thiazol-2-yl)-phosphonates with various substituents in positions 3, 4, and 5 of the thiazole ring wereprepared. However, only phosphonates with an aryl on the nitrogen atom were stable enoughfor chromatographic purification, although all the new phosphonates...
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Synthesis of Thermally Stable Energetic 1,2,3-Triazole Derivatives
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FUNKCJONALIZOWANIE 2H-TIAZOLO[3,2-α]PIRYDYN-5-(3H)-ONÓW, ALTERNATYWNA ŚCIEŻKA SYNTEZY NOWYCH PILICYDÓW
PublicationUropatogenne szczepy Escherichia coli są przyczyną blisko 80% przypadków zakażeń dróg moczowych (ang. UTI- Urinary tract infection). Ponadto, aż 30% odmiedniczkowego zapalenia nerek występującego u ciężarnych kobiet jest spowodowane przez szczepy E.coli Dr+. Szerząca się lekooporność bakterii i trudności w leczeniu UTI wymusiły na środowiskach naukowych poszukiwania nowych związków chemicznych pełniących rolę chemoterapeutyków. Na...
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Aromatic heptaene antibiotics as an alternative for synthetic triazole fungicides in plant protection
PublicationAn in vitro antifungal activity of candicidin and ascosin antibiotics (0,01-10 μg/mL) towards representative strains of phytopathogenic fungi was detd. Both compds. exhibited similar half max. effective concns. inhibiting growth of the fungi as that of tebuconazole used for comparison.
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New potent STS inhibitors based on fluorinated 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates
PublicationA series of fluorinated analogs based on the frameworks of 4-(1- phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamates have been synthesized as steroid sulfatase (STS) inhibitors. The design of chemical structures of new potential STS inhibitors was supported by molecular docking techniques to identify potential interactions between inhibitors and amino acid residues located in the STS active site. The STS inhibitory potency was evaluated...
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Activity of isavuconazole and other triazole derivatives against clinical isolates of Aspergillus fumigatus
PublicationAspergillus fumigatus is the most frequent pathogen of the genus Asperillus, which is highly susceptible to triazole derivatives, especially to isavuconazole and voriconazole. Many countries face a growing problem of infections due to A. fumigatus showing acquired resistance to one or several triazoles. In medical centres, monitoring the susceptibility of isolated Aspergillus spp. is recommended. The aim of this study was to collect...
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Synthesis of Fentanyl Triazole Derivatives and their Affinity for Mu-Opioid and Sigma-1 Receptors
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The Effect of Posaconazole, Itraconazole and Voriconazole in the Culture Medium on Aspergillus fumigatus Triazole Resistance
PublicationTriazoles are the only compounds used as antibiotics in both medicine and agriculture. The presence of triazoles in the environment can contribute to the acquisition of azole resistance among isolates of Aspergillus fumigatus. The objective of this study was to investigate the effect of A. fumigatus exposure to triazoles on susceptibility to these compounds. Seventeen triazole-resistant and 21 triazole-sensitive A. fumigatus isolates...
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CLICK 'n' Sleep: Light-Switch Behavior of Triazole-Containing Tris(bipyridyl)ruthenium Complexes
PublicationA set of RuII complexes incorporating triazole subunits are presented. They show a solvent-dependent light-switch effect. Theoretical calculations revealed the excited states involved in the emission process. The findings are highly important for future design of light-switch sensors and suggest a severe restriction for functional photomolecular devices synthesized by CLICK chemistry.
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublicationIn the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...