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21.
Giovanni Petrillo Cinzia Tavani Lara Bianchi Alice Benzi Maria Maddalena Cavalluzzi Lara Salvagno Laura Quintieri Annalisa De Palma Leonardo Caputo Antonio Rosato Giovanni Lentini 《Molecules (Basel, Switzerland)》2021,26(13)
Twenty-two novel, variously substituted nitroazetidines were designed as both sulfonamide and urethane vinylogs possibly endowed with antimicrobial activity. The compounds under study were obtained following a general procedure recently developed, starting from 4-nitropentadienoates deriving from a common β-nitrothiophenic precursor. While being devoid of any activity against fungi and Gram-negative bacteria, most of the title compounds performed as potent antibacterial agents on Gram-positive bacteria (E. faecalis and three strains of S. aureus), with the most potent congener being the 1-(4-chlorobenzyl)-3-nitro-4-(p-tolyl)azetidine 22, which displayed potency close to that of norfloxacin, the reference antibiotic (minimum inhibitory concentration values 4 and 1–2 μg/mL, respectively). Since 22 combines a relatively efficient activity against Gram-positive bacteria and a cytotoxicity on eucharyotic cells only at 4-times higher concentrations (inhibiting concentration on 50% of the cultured eukaryotic cells: 36 ± 10 μM, MIC: 8.6 μM), it may be considered as a promising hit compound for the development of a new series of antibacterials selectively active on Gram-positive pathogens. The relatively concise synthetic route described herein, based on widely available starting materials, could feed further structure–activity relationship studies, thus allowing for the fine investigation and optimization of the toxico-pharmacological profile. 相似文献
22.
Giuseppe Cremonesi Piero Dalla Croce Alessandra Forni Maddalena Gallanti Raffaella Gandolfi Concetta La Rosa 《Tetrahedron: Asymmetry》2009,20(16):1940-1947
Enantiomerically pure (5R)-(?)-5-phenyl-4,5-dihydroisoxazole-3-carboxylic acid ethyl ester was obtained via enzymatic resolution of the corresponding racemic mixture using a lipase from hog pancreas (PPL). The following reduction of the ester group to the corresponding alcohol and the oxidation of the latter led to (5R)-(?)-5-phenyl-4,5-dihydroisoxazole-3-carbaldehyde, and the reaction between this and Schöllkopf’s reagent, (2R)-(+)-2,5-dihydro-3,6-dimethoxy-2-isopropylpyrazine, gave mixtures of adducts with a good syn/anti ratio. The steric configurations of the major diastereoisomer were assigned on the basis of spectroscopic data and X-ray analysis. The subsequent controlled hydrolysis of the pyrazine ring led to β-(5-phenyl-4,5-dihydroisoxazol-3-yl)-serine methyl esters and the corresponding dipeptides with (R)-valine. Finally, reductive cleavage of the 4,5-dihydroisoxazole ring under hydrolytic conditions made it possible to obtain the corresponding polyfunctionalised dipeptides. 相似文献
23.
24.
G. Di Francia V. La Ferrara P. Maddalena D. Ninno L. P. Odierna V. Cataudella 《Il Nuovo Cimento D》1996,18(10):1187-1196
Summary In this paper we report on the frequency dependence of the AC conductivity of porous silicon in the range 10 Hz-100 kHz. Two
types of testing devices have been fabricated on three different series of samples formed electrochemically using as a starting
materialptype,n
−-type andn
+-type silicon substrates. For frequencies less than 20-40 kHz the conductivity is found to follow a sublinear frequency dependence.
This behaviour is typical of a carrier transport mechanism determined by an anomalous diffusion process. At higher frequencies
we find that surface states influence the transport mechanism. This suggests a double-channel transport mechanism: one related
to porous-silicon “volume” properties and the other more connected to the “surface” itself.
Paper presented at the III INSEL (Incontro Nazionale sul Silicio Emettiore di Luce) Torino, 12–13 October 1995. 相似文献
25.
Des Mazery R Pullez M López F Harutyunyan SR Minnaard AJ Feringa BL 《Journal of the American Chemical Society》2005,127(28):9966-9967
A highly enantioselective (up to 96% ee) conjugate addition of Grignard reagents, in particular, MeMgBr, to alpha,beta-unsaturated thioesters is provided as well as its application to a diastereo- and enantioselective iterative route to syn- and anti-1,3-dimethyl arrays and deoxypropionate subunits. The versatility of the method is illustrated in the synthesis of (-)-lardolure, a multimethyl-branched insect natural pheromone. 相似文献
26.
Serena Traboni Emiliano Bedini Maddalena Giordano Alfonso Iadonisi 《Tetrahedron letters》2019,60(27):1777-1780
A varied set of solvent-free, one-pot synthetic sequences were developed to carry out the orthogonal protection of saccharide polyols. These sequences are composed of an initial regioselective benzylation, silylation or iodination (under mildly basic conditions), followed by an acid catalyzed protection of two further hydroxyl sites via the generation of a cyclic acetal. These processes allow recycling of the ammonium or pyridinium side products generated in the former step as effective catalytic species for the latter step. 相似文献
27.
Coclite Giuseppe Maria Dipierro Serena Maddalena Francesco Valdinoci Enrico 《Journal of Nonlinear Science》2020,30(4):1285-1305
The formation of singularities in finite time in nonlocal Burgers’ equations, with time-fractional derivative, is studied in detail. The occurrence of finite-time singularity is proved, revealing the underlying mechanism, and precise estimates on the blowup time are provided. The employment of the present equation to model a problem arising in job market is also analyzed.
相似文献28.
Giuseppe Chirico Prof. Maddalena Collini Prof. Laura D'Alfonso Prof. Franck Denat Prof. Yuri A. Diaz‐Fernandez Dr. Luca Pasotti Dr. Yoann Rousselin Dr. Nicolas Sok Dr. Piersandro Pallavicini Prof. 《Chemphyschem》2008,9(12):1729-1737
Potentiometric titrations, fluorescence versus pH titrations, dynamic light scattering and fluorescence polarization anisotropy studies demonstrate that inside the nanodimensioned Triton X‐100 micelles, 1‐pyrenecarboxylic acid, PCOO?, forms an apical complex with the Zn2+ cation encircled by a lipophilic cyclen ligand and hugely increasing its fluorescence. The ability of the Zn2+‐cyclen‐PCOO? complex plus its micellar container to act as a fluorescent sensor to evaluate the lipophilicity of molecular species is demonstrated on the fatty acid series CH3(CH2)xCOOH (x=0–16). At pH 7.4 a decrease in fluorescence is observed on the addition of fatty acids that is directly related to their chain length, that is, to their tendency to enter the micellar containers, where they dislocate PCOO? from the Zn2+ centre. The independent determination of fatty acid pKa values in the presence of Triton X‐100 micelles confirms that our fluorescent micellar device is capable of sensing their lipophilicity. 相似文献
29.
Hydroxycinnamic acids derivatives, monomeric and oligomeric flavan-3-ols, flavonols, and dihydrocalcones are four of the major polyphenolic groups found in apples leaves and peels. A simple extraction with minimal pre-treatment and a high-performance liquid chromatography-diode array detection determination are optimized and validated, in order to identify and quantitate the polyphenolic profile of leaves and peels of four apples varieties (Gala, Topaz, Golden Delicious, and Florina). The improved chromatographic method has led to better separation of some known polyphenols in a single course, and diode-array detection has been used for the previsional identification of some polyphenolic compounds not available as standards. Because the mobile phase and the chromatographic column are compatible with a mass spectrometer, this method could investigate the unknown flavanols, flavonols, hydrocinnamic acid derivatives, and chalcone-related compounds found in apple leaves and peel extracts analyzed. 相似文献
30.
Mohamad Sleiman Randy L. Maddalena Lara A. Gundel Hugo Destaillats 《Journal of chromatography. A》2009,1216(45):7899-7905
Tobacco-specific nitrosamines (TSNAs) are some of the most potent carcinogens in tobacco and cigarette smoke. Accurate quantification of these chemicals is needed to help assess public health risks. We developed and validated a specific and sensitive method to measure four TSNAs adsorbed to model surfaces and secondhand smoke (SHS) particles using gas chromatography–ion-trap tandem mass spectrometry. In an 18-m3 room-sized chamber, a smoking machine generated realistic concentrations of SHS that were actively sampled on Teflon-coated fiber glass (TCFG) filters, and passively sampled on cellulose substrates. A simple solid–liquid extraction protocol using methanol as solvent was successfully applied to both substrates with recoveries ranging from 85 to 115%. For each TSNA, tandem MS parameters were optimized and the major fragmentation pathways were elucidated. The method showed excellent performance, with a linear dynamic range from 2 to 1000 ng mL−1, low detection limits (S/N > 3) of 30–300 pg mL−1 and precision with experimental errors below 10% for all compounds. Moreover, no interfering peaks were observed, indicating a high selectivity of MS/MS without the need for a sample clean-up step. This method provides a suitable analytical tool to detect and quantify traces of TSNA in indoor environments polluted with SHS. 相似文献