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21.
Makhluf J. Haddadin Claudia El-Nachef Yara Chaaban James C. Fettinger 《Tetrahedron letters》2010,51(51):6687-6689
Synthesis of the strained 2H-thieto[3,2-b]quinoline ring system is reported for the first time. Treatment of (Z)-2-benzyliden-2H-thieto[3,2-b]quinoline derivatives of this heterocycle with base, at reflux in ethanol, causes a novel rearrangement to 2-phenylthieno[3,2-b]quinolines. Indeed, the one-pot reaction of 2-aminobenzaldehydes and (Z)-2-benzylidenethietan-3-one in refluxing basic ethanol leads directly to 2-phenylthieno[3,2-b]quinolines in good yields. 相似文献
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Yara Santiago de Oliveira Wendell Saraiva Costa Poliana Ferreira Borges Maria Silmara Alves de Santana Alejandro Pedro Ayala 《Acta Crystallographica. Section C, Structural Chemistry》2019,75(5):483-495
The use of supramolecular synthons as a strategy to control crystalline structure is a crucial factor in developing new solid forms with physicochemical properties optimized by design. However, to achieve this objective, it is necessary to understand the intermolecular interactions in the context of crystal packing. The feasibility of a given synthon depends on its flexibility to combine the drug with a variety of coformers. In the present work, the imidazole–hydroxy synthon is investigated using as the target molecule benzoylmetronidazole [BZMD; systematic name 2‐(2‐methyl‐5‐nitro‐1H‐imidazol‐1‐yl)ethyl benzoate], whose imidazole group seems to be a suitable acceptor for hydrogen bonds. Thus, coformers with carboxylic acid and phenol groups were chosen. According to the availability of binding sites presented in the coformer, and considering the proposed synthon and hydrogen‐bond complementarity as major factors, different drug–coformer stoichiometric ratios were explored (1:1, 2:1 and 3:1). Thirteen new solid forms (two salts and eleven cocrystals) were produced, namely BZMD–benzoic acid (1/1), C13H13N3O4·C7H6O2, BZMD–β‐naphthol (1/1), C13H13N3O4·C10H8O, BZMD–4‐methoxybenzoic acid (1/1), C13H13N3O4·C8H8O3, BZMD–3,5‐dinitrobenzoic acid (1/1), C13H13N3O4·C7H4N2O6, BZMD–3‐aminobenzoic acid (1/1), C13H13N3O4·C7H7NO2, BZMD–salicylic acid (1/1), C13H13N3O4·C7H6O3, BZMD–maleic acid (1/1) {as the salt 1‐[2‐(benzoyloxy)ethyl]‐2‐methyl‐5‐nitro‐1H‐imidazol‐3‐ium 3‐carboxyprop‐2‐enoate}, C13H14N3O4+·C4H3O4?, BZMD–isophthalic acid (1/1), C13H13N3O4·C8H6O4, BZMD–resorcinol (2/1), 2C13H13N3O4·C6H6O2, BZMD–fumaric acid (2/1), C13H13N3O4·0.5C4H4O4, BZMD–malonic acid (2/1), 2C13H13N3O4·C3H2O4, BZMD–2,6‐dihydroxybenzoic acid (1/1) {as the salt 1‐[2‐(benzoyloxy)ethyl]‐2‐methyl‐5‐nitro‐1H‐imidazol‐3‐ium 2,6‐dihydroxybenzoate}, C13H14N3O4+·C7H5O4?, and BZMD–3,5‐dihydroxybenzoic acid (3/1), 3C13H13N3O4·C7H6O4, and their crystalline structures elucidated, confirming the robustness of the selected synthon. 相似文献
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Yara M. Gomes 《Applied biochemistry and biotechnology》1997,66(2):107-119
In the acute phase of Chagas’ disease, when the parasitemia is high, diagnosis can be easily made using conventional parasitological
methods. During the chronic phase, due to the low parasitemia, diagnosis is performed mainly by immunological methods. Conventional
serological techniques are limited by cross-reactivity with other parasitic diseases, non-standardization of reagents, and
the diversity of technical procedures. Methods are being developed to improve the sensitivity and specificity of diagnosis
using molecular approaches. PCR-based detection systems and the use of recombinant antigens in ELISA are the most promising. 相似文献
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2(3),9(10),16(17),23(24)-Tetrakis-4′-[3,5-bis-(trifluoromethyl)-phenoxy]-phthalocyanines, {M[Pc-β(OBz-(CF3)2)4]}, (M = Zn(II), Cu(II), Co(II) and Ni(II)) were synthesized and characterized by elemental analysis, FTIR, 1H NMR, UV–Vis and MS (Maldi-TOF) spectral data. It is shown that the 4-(3,5-bis(trifluoromethyl)-phenoxy) moieties on the periphery affect the solubility, spectroscopic data and electrochemistry of the tetrakis metallophthalocyanines. The cyclic voltammetry and differential pulsed voltammetry of the complexes give well-defined redox couples in harmony with common metallophthalocyanine complexes. Electrochemical studies show that the complexes exhibit stable monoanionic M{Pc-β-[(OBz-(CF3)2)4]}1−, dianionic M{Pc-β-[(OBz-(CF3)2)4]}2− and monocationic M{Pc-β-[(OBz-(CF3)2)4]}1+ species during the reduction and oxidation processes. When compared with the unsubstituted analogues, the redox potentials of the complexes shifted to more positive potentials due to the electron-withdrawing fluorine groups. 相似文献
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Dumat B Bordeau G Aranda AI Mahuteau-Betzer F El Harfouch Y Metgé G Charra F Fiorini-Debuisschert C Teulade-Fichou MP 《Organic & biomolecular chemistry》2012,10(30):6054-6061
On the basis of our previous work on vinyl-triphenylamine derived DNA fluorophores we explored the structure space around this core by coupling it to diverse cationic, anionic and zwitterionic groups in the aim of targeting different classes of biomolecules. In parallel core modifications were performed to optimize the photophysical properties (quantum yield, two-photon absorption). The resulting water soluble π-conjugated molecules are called TP dyes and display an exceptional combination of optical properties: high two-photon absorption cross-section, high photostability, no self-quenching, and switchable fluorescence emission when bound to a biopolymer matrix. The linear and nonlinear optical properties of the TP dyes were studied in vitro in presence of DNA and in presence of a model protein (human serum albumin) using complementary absorption and fluorescence spectroscopy characterization tools. Structure modifications enabled to switch from DNA probes (cationic TP-pyridinium series) to protein probes (anionic TP-rhodanine series) without affecting the optical properties. Finally most TP compounds appear cell-permeant and show an intracellular localization consistent with their in vitro target specificity. 相似文献
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Samir Mohamed Awad Shima Mahmoud Ali Yara Essam Mansour Samar Said Fatahala 《Molecules (Basel, Switzerland)》2021,26(10)
Since herpes simplex virus type 1 (HSV-1) infection is so widespread, several antiviral drugs have been developed to treat it, among which are uracil nucleosides. However, there are major problems with the current medications such as severe side-effects and drug resistance. Here we present some newly synthesized cyclic and acyclic uracil nucleosides that showed very promising activity against HSV-1 compared to acyclovir. 相似文献
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Light‐mediated DNA Repair Prevents UVB‐induced Cell Cycle Arrest in Embryos of the Crustacean Macrobrachium olfersi 下载免费PDF全文
Eliane Cristina Zeni Dib Ammar Mayana Lacerda Leal Heloisa Schramm da Silva Silvana Allodi Yara Maria Rauh Müller Evelise Maria Nazari 《Photochemistry and photobiology》2015,91(4):869-878
High levels of ultraviolet‐B (UVB) radiation can negatively affect aquatic animals. Macrobrachium olfersi is a prawn that lives in clear freshwaters and during the breeding season, females carry eggs in an external brood pouch. Therefore, we hypothesize that eggs are also exposed to environmental UVB radiation. The aim of this study was to investigate whether UVB radiation induces DNA damage and compromises cell cycle in embryos of M. olfersi. In laboratory, UVB irradiance (310 mW. cm?2) that embryos receive in the natural environment was simulated. After irradiation, embryos were kept under different light conditions in order to recognize the presence of cell repair. UVB radiation induces DNA damage, specifically thymine dimers. After 48 h of UVB exposure, a significant decrease in the level of these dimers was observed in embryos kept under visible light while it remained constant in the dark. Moreover, under visible light and darkness, a decrease in proliferation was observed after 48 h of irradiation. An increase in PCNA expression and decrease in p53 expression were observed after, respectively, 1 and 48 h of exposure. Our results showed that UVB radiation disturbs the cell cycle and induces DNA damage in M. olfersi embryos. However, under visible light these embryos showed successful DNA repair. 相似文献