52780-23-1Relevant academic research and scientific papers
Design, synthesis, and evaluation of compounds capable of reducing Pseudomonas aeruginosa virulence
Hossain, Mohammad Anwar,Sattenapally, Narsimha,Parikh, Hardik I.,Li, Wei,Rumbaugh, Kendra P.,German, Nadezhda A.
supporting information, (2019/11/26)
Anti-virulence approaches in the treatment of Pseudomonas aeruginosa (PA)-induced infections have shown clinical potential in multiple in vitro and in vivo studies. However, development of these compounds is limited by several factors, including the lack of molecules capable of penetrating the membrane of gram-negative organisms. Here, we report the identification of novel structurally diverse compounds that inhibit PqsR and LasR-based signaling and diminish virulence factor production and biofilm growth in two clinically relevant strains of P. aeruginosa. It is the first report where potential anti-virulent agents were evaluated for inhibition of several virulence factors of PA. Finally, co-treatment with these inhibitors significantly reduced the production of virulence factors induced by the presence of sub-inhibitory levels of ciprofloxacin. Further, we have analyzed the drug-likeness profile of designed compounds using quantitative estimates of drug-likeness (QED) and confirmed their potential as hit molecules for further development.
Compound for organic photoelectric device, organic photoelectric device, and display device
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Paragraph 0152-0156, (2020/12/30)
Disclosed are a compound for an organic photoelectric device represented by a combination of Chemical Formula 1 and Chemical Formula 2, an organic photoelectric device including the compound, and a display device. Details of Chemical Formula 1 and Chemica
COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, COMPOSITION FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE
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Paragraph 0096, (2019/11/27)
Disclosed are a compound for an organic optoelectronic device, a composition for an organic optoelectronic device including the same, an organic optoelectronic device including the composition for an organic optoelectronic device as a host, and a display
A Revised Modular Approach to (–)-trans-Δ8-THC and Derivatives Through Late-Stage Suzuki–Miyaura Cross-Coupling Reactions
Bloemendal, Victor R. L. J.,Sondag, Daan,Elferink, Hidde,Boltje, Thomas J.,van Hest, Jan. C. M.,Rutjes, Floris P. J. T.
, p. 2289 - 2296 (2019/04/03)
A revised modular approach to various synthetic (–)-trans-Δ8-THC derivatives through late-stage Suzuki–Miyaura cross-coupling reactions is disclosed. Ten derivatives were synthesized allowing both sp2- and sp3-hybridized cross-coupling partners with minimal β-hydride elimination. Importantly, we demonstrate that a para-bromo-substituted THC scaffold for Suzuki–Miyaura cross-coupling reactions has been initially reported incorrectly in recent literature.
COMPOUND, COMPOSITION AND ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE
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Paragraph 0283-0286, (2019/12/31)
The present invention relates to a compound represented by a combination of chemical formula 1 and chemical formula 2, a composition including the compound, an organic optoelectronic device, and a display device. In the chemical formula 1 and chemical for
Controlled Generation of 3-Triflyloxyarynes
Uchida, Keisuke,Yoshida, Suguru,Hosoya, Takamitsu
supporting information, p. 4099 - 4109 (2016/11/26)
The efficient generation of 3-triflyloxyarynes, including those bearing a transformable group, through an iodine-magnesium exchange reaction of 1,3-bis(triflyloxy)-2-iodoarenes was achieved by using finely tuned reaction conditions that efficiently suppre
BROMODOMAIN INHIBITORS FOR TREATING DISEASE
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Paragraph 0233-0234, (2016/03/19)
Disclosed herein are compounds and compositions useful in the treatment of bromodomain-containing protein-mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibiting activity of a bromodomain-containing protein in a human or animal subject are also provided.
Biocatalytic Properties and Structural Analysis of Phloroglucinol Reductases
Conradt, David,Hermann, Bianca,Gerhardt, Stefan,Einsle, Oliver,Müller, Michael
supporting information, p. 15531 - 15534 (2016/12/09)
Phloroglucinol reductases (PGRs) are involved in anaerobic degradation in bacteria, in which they catalyze the dearomatization of phloroglucinol into dihydrophloroglucinol. We identified three PGRs, from different bacterial species, that are members of the family of NAD(P)H-dependent short-chain dehydrogenases/reductases (SDRs). In addition to catalyzing the reduction of the physiological substrate, the three enzymes exhibit activity towards 2,4,6-trihydroxybenzaldehyde, 2,4,6-trihydroxyacetophenone, and methyl 2,4,6-trihydroxybenzoate. Structural elucidation of PGRcl and comparison to known SDRs revealed a high degree of conservation. Several amino acid positions were identified as being conserved within the PGR subfamily and might be involved in substrate differentiation. The results enable the enzymatic dearomatization of monoaromatic phenol derivatives and provide insight into the functional diversity that may be found in families of enzymes displaying a high degree of structural homology.
3-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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Page/Page column 93, (2010/04/06)
The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
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Page/Page column 34, (2009/12/23)
The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
