33265-60-0Relevant articles and documents
Synthesis of new piperazinyl-pyrrolo[1,2-: A] quinoxaline derivatives as inhibitors of Candida albicans multidrug transporters by a Buchwald-Hartwig cross-coupling reaction
Guillon, Jean,Nim, Shweta,Moreau, Stéphane,Ronga, Luisa,Savrimoutou, Solène,Thivet, Elisabeth,Marchivie, Mathieu,Di Pietro, Attilio,Prasad, Rajendra,Le Borgne, Marc
, p. 2915 - 2931 (2020)
Two series of piperazinyl-pyrrolo[1,2-a]quinoxaline derivatives were prepared via a Buchwald-Hartwig cross-coupling reaction and then evaluated for their ability to inhibit the drug efflux activity of CaCdr1p and CaMdr1p transporters of Candida albicans overexpressed in a Saccharomyces cerevisiae strain. In the initial screening of twenty-nine piperazinyl-pyrrolo[1,2-a]quinoxaline derivatives, twenty-three compounds behaved as dual inhibitors of CaCdr1p and CaMdr1p. Only four compounds showed exclusive inhibition of CaCdr1p or CaMdr1p. Further biological investigations were developed and for example, their antifungal potential was evaluated by measuring the growth of control yeast cells (AD1-8u-) and efflux pump-overexpressing cells (AD-CDR1 and AD-MDR1) after exposition to variable concentrations of the tested compounds. The MIC80 values of nineteen compounds ranging from 100 to 901 μM for AD-CDR1 demonstrated that relative resistance index (RI) values were between 8 and 274. In comparison, only seven compounds had RI values superior to 4 in cells overexpressing Mdr1p. These results indicated substrate behavior for nineteen compounds for CaCdr1p and seven compounds for CaMdr1p, as these compounds were transported via MDR transporter overexpressing cells and not by the AD1-8u- cells. Finally, in a combination assay with fluconazole, two compounds (1d and 1f) have shown a synergistic effect (fractional inhibitory concentration index (FICI) values ≤ 0.5) at micromolar concentrations in the AD-MDR1 yeast strain overexpressing CaMdr1p-protein, indicating an excellent potency toward chemosensitization.
PEG-400 as a carbon synthon: Highly selective synthesis of quinolines and methylquinolines under metal-free conditions
Ding, Chengcheng,Feng, Kaili,Li, Shichen,Ma, Chen
supporting information, p. 5542 - 5548 (2021/08/16)
A metal-free, peroxide-free, and efficient procedure for the highly selective synthesis of quinolines and methylquinolines was reported. The main feature of this method was that the same substrate can produce quinolines and methylquinolines, respectively, under different reaction conditions. PEG-400 was used as both a reactant and solvent in this reaction. The utility of the designed procedure was also demonstrated by the derivatization of the products to bioactive compounds. This journal is
Pyrrolyl group-containing compound, polymer, mixture, composition, and organic electronic device
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Paragraph 0168-0173; 0180-0185, (2020/11/26)
The invention discloses a pyrrolyl-containing compound, a high polymer, a mixture, a composition and an organic electronic device. The pyrrolyl-containing compound contains a structure represented bya general formula (1), forms a condensed ring with other functional units through a pyrrolyl group, and is adjusted in the aspects of molecular stability and transmission performance. The pyrrolyl-containing compound disclosed by the invention is used in an OLED, particularly used as a light emitting layer material, and can provide higher device performance.