102852-93-7Relevant academic research and scientific papers
Redesigning of the cap conformation and symmetry of the diphenylethyne core to yield highly potent pan-genotypic NS5A inhibitors with high potency and high resistance barrier
Abdallah, Mennatallah,Hamed, Mostafa M.,Frakolaki, Efseveia,Katsamakas, Sotirios,Vassilaki, Niki,Bartenschlager, Ralf,Zoidis, Grigoris,Hirsch, Anna K.H.,Abdel-Halim, Mohammad,Abadi, Ashraf H.
, (2021/12/27)
Herein, we report the discovery of several NS5A inhibitors with potency against HCV genotype 1b in the picomolar range. Compounds (15, 33) were of extremely high potency against HCV genotype 1b (EC50 ≈ 1 pM), improved activity against genotype 3a (GT 3a) and good metabolic stability. We studied the impact of changing the cap conformation relative to the diphenylethyne core and/or compound symmetry on both potency and metabolic stability. The analogs obtained exhibited improved potency against HCV genotypes 1a, 1b, 3a and 4a compared to the clinically approved candidate daclatasvir with EC50 values in the low picomolar range and SI50s > 7 orders of magnitude. Compound 15, a symmetrically m-, m’-substituted diphenyl ethyne analog, was 150-fold more potent than daclatasvir against GT 3a, while compound 33, an asymmetrically m-, p-substituted diphenyl ethyne analog, was 35-fold more potent than daclatasvir against GT 3a. In addition, compound 15 exhibited a higher resistance barrier than daclatasvir against genotype 1b.
Carborane-perylene diimide derivative and synthesis method thereof, sensing array based on derivative and preparation method and application of sensor array
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Paragraph 0111; 0114; 0115; 0116; 0157, (2018/04/02)
The invention discloses a carborane-perylene diimide derivative and a synthesis method thereof, a sensing array based on the derivative and a preparation method and an application of the sensor array,and belongs to the technical field of small-molecular fluorescent sensing thin film materials. The carborane-perylene diimide derivative is placed in a solution, is assembled into a fiber structure with relatively large specific surface, and then is transferred to different substrate surfaces, so as to obtain the sensing array composed of a variety of fluorescent thin films; the sensing array canbe sensitive to sense six important drug gases, and drug samples have no need of any treatment; at the same time, through array combination, the interference of common interferents is eliminated thoroughly. The operation is simple, and the reaction conditions are mild. The prepared fluorescent sensing thin film has good stability and long service life, and is an excellent drug gas sensing thin film array. With combination use of the thin film and commercial fluorescent instruments, the drug gases can be sensitively detected. In addition, the drug gas special detection instrument can be developed through the device of the sensing thin film.
Magnetic interaction between the triplet centers in ethynylenebis(phenylnitrenes) and 1,3-butadiyne-1,4-diylbis(phenylnitrenes)
Murata, Shigeru,Iwamura, Hiizu
, p. 5547 - 5556 (2007/10/02)
The magnetic interaction of the two triplet phenylnitrene units linked together through an acetylene or a diacetylene linkage has been investigated by ESR spectroscopy. Two regioisomeric (meta,para′ and meta, meta′) diazides of 1,2-diphenylacetylene 12a a
