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Mihaela Badea Rodica Olar Valentina Uivarosi Dana Marinescu Victoria Aldea Stefania Felicia Barbuceanu George Mihai Nitulescu 《Journal of Thermal Analysis and Calorimetry》2011,105(2):559-564
Two new complexes having general formula VOL2·nH2O [(1) L: 5-hydroxyflavone, n = 1; (2) L: chrysin, n = 4] were synthesized and characterized. Based on IR and electronic data we concluded that studied flavones act as bidentate
ligands in complexes with metallic ion coordinated in a square-pyramidal stereochemistry. The thermal analysis (TG, DTA) elucidated
the composition and also the number and nature of the water molecules. The thermal behavior also indicated strong interactions
between oxovanadium (IV) and these oxygen donor ligands. 相似文献
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Stefania‐Felicia Barbuceanu Gabriela Bancescu Gabriel Saramet Florica Barbuceanu Constantin Draghici Flavian Stefan Radulescu Aura Ionescu Simona Negres 《Heteroatom Chemistry》2013,24(4):309-321
In the present study, new 1,2,4‐triazoles, 1,3,4‐thiadiazoles, and acylthiosemicarbaz‐ides derived from 4‐(4‐chlorophenylsulfonyl)benzoic acid hydrazide were synthesized and screened for their antimicrobial and analgesic activities. Acylthiosemicarbazides 2–4 were synthesized by a reaction of 4‐(4‐chlorophenyl‐sulfonyl)benzoic acid hydrazide 1 with different arylisothiocyanates.4,5‐Disubstituted‐2,4‐dihydro‐3H‐1,2,4‐triazol‐3‐thiones 5–7 and 2,5‐disubstituted‐1,3,4‐thiadiazoles 8–10 were obtained by dehydrative cyclization of corresponding acylthiosemicarbazide derivatives 2–4 in basic media (8% aqueous sodium hydroxide) and in acidic media (sulfuric acid or phosphorous oxychloride), respectively. The structures of the newly synthesized compounds have been confirmed on the basis of elemental analysis and spectral studies (IR, 1H NMR, 13C NMR, MS). Their antimicrobial activities against some bacteria and yeasts were investigated. The analgesic activity of all compounds was performed with two pharmacological tests: the writhing test induced with acetic acid and hot‐plate test. The results showed that triazole 7 had the best antimicrobial activity against Bacillus cereus. In the chemical stimulus test, triazoles 6 and 7 were the most active compounds whereas in the hot‐plate test thiadiazoles 9 and 10 exhibited the highest analgesic activity. 相似文献
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Theodora-Venera Apostol Luminita Gabriela Marutescu Constantin Draghici Laura-Ileana Socea Octavian Tudorel Olaru George Mihai Nitulescu Elena Mihaela Pahontu Gabriel Saramet Cristian Enache-Preoteasa Stefania-Felicia Barbuceanu 《Molecules (Basel, Switzerland)》2021,26(16)
In order to develop novel bioactive substances with potent activities, some new valine-derived compounds incorporating a 4-(phenylsulfonyl)phenyl fragment, namely, acyclic precursors from N-acyl-α-amino acids and N-acyl-α-amino ketones classes, and heterocycles from the large family of 1,3-oxazole-based compounds, were synthesized. The structures of the new compounds were established using elemental analysis and spectral (UV-Vis, FT-IR, MS, NMR) data, and their purity was checked by reversed-phase HPLC. The newly synthesized compounds were evaluated for their antimicrobial and antibiofilm activities, for toxicity on D. magna, and by in silico studies regarding their potential mechanism of action and toxicity. The 2-aza-3-isopropyl-1-[4-(phenylsulfonyl)phenyl]-1,4-butanedione 4b bearing a p-tolyl group in 4-position exhibited the best antibacterial activity against the planktonic growth of both Gram-positive and Gram-negative strains, while the N-acyl-α-amino acid 2 and 1,3-oxazol-5(4H)-one 3 inhibited the Enterococcus faecium biofilms. Despite not all newly synthesized compounds showing significant biological activity, the general scaffold allows several future optimizations for obtaining better novel antimicrobial agents by the introduction of various substituents on the phenyl moiety at position 5 of the 1,3-oxazole nucleus. 相似文献
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Theodora-Venera Apostol Mariana Carmen Chifiriuc Constantin Draghici Laura-Ileana Socea Luminita Gabriela Marutescu Octavian Tudorel Olaru George Mihai Nitulescu Elena Mihaela Pahontu Gabriel Saramet Stefania-Felicia Barbuceanu 《Molecules (Basel, Switzerland)》2021,26(16)
The multi-step synthesis, physico-chemical characterization, and biological activity of novel valine-derived compounds, i.e., N-acyl-α-amino acids, 1,3-oxazol-5(4H)-ones, N-acyl-α-amino ketones, and 1,3-oxazoles derivatives, bearing a 4-[(4-chlorophenyl)sulfonyl]phenyl moiety are reported here. The structures of the newly synthesized compounds were confirmed by spectral (UV-Vis, FT-IR, MS, 1H- and 13C-NMR) data and elemental analysis results, and their purity was determined by RP-HPLC. The new compounds were assessed for their antimicrobial activity and toxicity to aquatic crustacean Daphnia magna. Also, in silico studies regarding their potential mechanism of action and toxicity were performed. The antimicrobial evaluation revealed that the 2-{4-[(4-chlorophenyl)sulfonyl]benzamido}-3-methylbutanoic acid and the corresponding 1,3-oxazol-5(4H)-one exhibited antimicrobial activity against Gram-positive bacterial strains and the new 1,3-oxazole containing a phenyl group at 5-position against the C. albicans strain. 相似文献
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Beatrice-Cristina Ivan Florea Dumitrascu Adriana Iuliana Anghel Robert Viorel Ancuceanu Sergiu Shova Denisa Dumitrescu Constantin Draghici Octavian Tudorel Olaru George Mihai Nitulescu Mihaela Dinu Stefania-Felicia Barbuceanu 《Molecules (Basel, Switzerland)》2021,26(21)
A series of new pyrrole derivatives were designed as chemical analogs of the 1,4-dihydropyridines drugs in order to develop future new calcium channel blockers. The new tri- and tetra-substituted N-arylpyrroles were synthesized by the one-pot reaction of 1-methyl-3-cyanomethyl benzimidazolium bromide with substituted alkynes having at least one electron-withdrawing substituent, in 1,2-epoxybutane, acting both as the solvent and reagent to generate the corresponding benzimidazolium N3-ylide. The structural characterization of the new substituted pyrroles was based on IR, NMR spectroscopy as well as on single crystal X-ray analysis. The toxicity of the new compounds was assessed on the plant cell using Triticum aestivum L. species and on the animal cell using Artemia franciscana Kellogg and Daphnia magna Straus crustaceans. The compounds showed minimal phytotoxicity on Triticum rootlets and virtually no acute toxicity on Artemia nauplii, while on Daphnia magna, it induced moderate to high toxicity, similar to nifedipine. Our research indicates that the newly synthetized pyrrole derivatives are promising molecules with biological activity and low acute toxicity. 相似文献
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