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V. V. Kastron A. M. Kats G. Ya. Dubar R. M. Zolotoyabko 《Chemistry of Heterocyclic Compounds》1978,14(11):1236-1240
4,4-Disubstituted 1,4-dihydropyridines (I) are brominated with bromine in chloroform to give 2,6-bis(bromomethyl)-4,4-disubstituted 1,4-dihydropyridines (II), whereas 2,6-bis(dibromomethyl)-4,4-disubstituted 1,4-dihydropyridines (III) are obtained in the case of bromination of I in acetic acid. The bromine atoms in II and III are labile and readily undergo nucleophilic substitution.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1519–1524, November, 1978. 相似文献
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Puchi-Cabrera E.S. Guérin J.-D. La Barbera-Sosa J.G. Álvarez-Hostos J.C. Moreau P. Dubar M. Dubar L. 《Experimental Mechanics》2020,60(4):445-458
Experimental Mechanics - The experimental flow stress curves of structural steels obtained from axisymmetric compression tests conducted under hot-working conditions very often include the... 相似文献
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Martin C. Cooper Andreas Herzig Faustine Maffre Frédéric Maris Pierre Régnier 《Discrete Mathematics》2019,342(3):654-663
In the gossip problem information (‘secrets’) must be shared among a certain number of agents using the minimum number of calls. We extend the gossip problem to arbitrary epistemic depths. For example, we may require not only that all agents know all secrets but also that all agents know that all agents know all secrets. We give optimal protocols for various versions of this epistemic gossip problem, depending on the graph of communication links, in the case of two-way communication, one-way communication and parallel communication. We show, among other things, that increasing epistemic depth from 1 (all agents know all secrets) to 2 (so that all agents know that all agents know all secrets) does not double the required number of calls but increases this number by (for a complete graph). We also show that the following counter-intuitive result generalises to the epistemic gossip problem: asymptotically the same number of calls are required whether calls are two-way or one-way. 相似文献
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Georgiana Negru Laure Kamus Elena Bîcu Sergiu Shova Boualem Sendid Faustine Dubar Alina Ghinet 《Molecules (Basel, Switzerland)》2021,26(19)
The treatment of benzylidenemalononitriles with phenylhydrazines in refluxing ethanol did not provide pyrazole derivatives, but instead furnished hydrazones. The structure of hydrazones was secured by X-ray analysis. The chemical proof was also obtained by direct reaction of 3,4,5-trimethoxybenzaldehyde with 2,4-dichlorophenylhydrazine. Newly synthesized hydrazones were tested against eight Candida spp. strains in a dose response assay to determine the minimum inhibitory concentration (MIC99). Five compounds were identified as promising antifungal agents against Candida spp. (C. albicans SC5314, C. glabrata, C. tropicalis, C. parapsilosis and C. glabrata (R azoles)), with MIC99 values ranging from 16 to 32 µg/mL and selective antifungal activity over cytotoxicity. 相似文献
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Josefina Quirante Faustine Dubar Asensio González Marta Cascante Isabelle Forfar Christophe Biot 《Journal of organometallic chemistry》2011,696(5):1011-5432
We report the synthesis, characterization, and cytotoxic and antimalarial activity of ferrocene-indole hybrids 8-14. The 2-phenylindole scaffold was chosen because of its potent antimitotic activity and ferrocene was chosen following the development of ferrocifens, ferrocene derivatives of tamoxifen, which are prototypes of a new family of organometallic anti-estrogens. Ferrocene-indole hybrids 8-14 and their corresponding organic analogues 1-7 showed only moderate antimalarial activities, while ferrocene-indole hybrids 11 and 12 showed excellent in vitro activities against the A549 human carcinoma cell line, with IC50 values of 5 and 7 μM respectively. These ferrocene-indole hybrids were up to 25-fold more potent as cytotoxic agents than their purely organic analogues. 相似文献
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Dubar F Bohic S Slomianny C Morin JC Thomas P Kalamou H Guérardel Y Cloetens P Khalife J Biot C 《Chemical communications (Cambridge, England)》2012,48(6):910-912
We report here for the first time the in vitro localization of unlabeled antimalarial drugs with high spatial resolution. This strategy further enhances our understanding of the action mechanisms of antimalarial drugs. Our approach may be applied to a wide range of domains where quantitative chemical imaging of drugs at the sub-cellular level appears critical. 相似文献
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Dr. Jérôme de Ruyck Dr. Christian Dupont Elodie Lamy Dr. Vincent Le Moigne Prof. Christophe Biot Dr. Yann Guérardel Prof. Jean-Louis Herrmann Dr. Mickaël Blaise Dr. Stanislas Grassin-Delyle Dr. Laurent Kremer Dr. Faustine Dubar 《ChemistryOpen》2020,9(3):351-365
Non-tuberculous mycobacterium (NTM) infections, such as those caused by Mycobacterium abscessus, are increasing globally. Due to their intrinsic drug resistance, M. abscessus pulmonary infections are often difficult to cure using standard chemotherapy. We previously demonstrated that a piperidinol derivative, named PIPD1, is an efficient molecule both against M. abscessus and Mycobacterium tuberculosis, the agent of tuberculosis, by targeting the mycolic acid transporter MmpL3. These results prompted us to design and synthesize a series of piperidinol derivatives and to determine the biological activity against M. abscessus. Structure-activity relationship (SAR) studies pointed toward specific sites on the scaffold that can tolerate slight modifications. Overall, these results identified FMD-88 as a new promising active analogue against M. abscessus. Also, we determined the pharmacokinetics properties of PIPD1 and showed that intraperitoneal administration of this compound resulted in promising serum concentration and an elimination half-life of 3.2 hours. 相似文献
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Curis E Dubar F Nicolis I Bénazeth S Biot C 《The journal of physical chemistry. A》2012,116(23):5577-5585
Antimalarial compounds ruthenoquine and methylruthenoquine were studied by X-ray absorption spectroscopy both in solid state and in solution, in normal (aqueous or CH(2)Cl(2) solutions) and oxidative (aqueous solution with H(2)O(2), either equimolar or in large excess) conditions, to detect small changes in the coordination sphere of the ruthenium atom. Since changes in the EXAFS spectra of these compounds are quite subtle, a complete procedure was developed to assess the different sources of uncertainties in fitted structural parameters, including the use of multivariate statistic methods for simultaneous comparison of edge energy correction ΔE(0) and distances, which can take into account the very strong correlation between these two parameters. Factors limiting the precision of distance determination depend on the recording mode. In transmission mode, the main source of uncertainty is the data reduction process, whereas in fluorescence mode, experimental noise is the main source of variability in the fitted parameters. However, it was shown that the effects of data reduction are systematic and almost identical for all compounds; hence, they can be ignored when comparing distances. Consequently, for both fluorescence and transmission recorded spectra, experimental noise is the limiting factor for distance comparisons, which leads to the use of statistical methods for comparing distances. Univariate methods, focusing on the distance only, are shown to be less powerful in detecting changes in distances than bivariate methods making a simultaneous comparison of ΔE(0) and distances. This bivariate comparison can be done either by using the Hotelling's T(2) test or by using a graphical comparison of Monte Carlo simulation results. We have shown that using these methods allows for the detection of very subtle changes in distances. When applied to ruthenoquine compounds, it suggests that the implication of the nonbinding doublet of the aminoquine nitrogen in either protonation or methylation enhances the tilt of the two cyclopentadienyls. It also suggests that ruthenoquine and methylruthenoquine are, at least partially, oxidized in the presence of H(2)O(2), with a small decrease in the Ru-C bond length and increase in the edge energy. 相似文献