49629-37-0Relevant articles and documents
A class of 2-benzylene tetrahydronaphthalone derivatives and preparation methods and applications thereof
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Paragraph 0188-0192; 0208-0212, (2022/03/31)
The present invention relates to the field of biotechnology, discloses a class of 2-benzylene tetrahydrophthalone derivatives and preparation methods and applications thereof. 2-Benzylene tetrahydronaphthalone derivative having the following structural formula, wherein R1 is selected from chlorine, bromine, iodine, alkyl, alkoxy, substituted or unsubstituted amino, alkylthio, alkyneoxy, hydroxy or hydroxymethyl group; R2, R3, R4 are hydrogen or carboxyl-containing substituents, and R2, R3, or R4 At least one of them is a carboxyl-containing substituent group. The present invention innovatively proposes a class of 2-benzylene tetrahydronaphthalone derivatives as a new skeleton of firefly luciferase inhibitors. A class of 2-benzylene tetrahydronaphthone derivatives of the present invention having a highly efficient inhibitor of nanomolar and a nanamol IC50; by competing with D- fluorescein reversibly inhibits firefly luciferase, and exhibits a high effect of firefly glowworm luciferase inhibition at the enzyme, intracellular and in vivo levels; at the same time, it is shown that it has good biocompatibility and application potential.
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity
Abdel-Halim, Mohammad,Sigler, Sara,Racheed, Nora A. S.,Hefnawy, Amr,Fathalla, Reem K.,Hammam, Mennatallah A.,Maher, Ahmed,Maxuitenko, Yulia,Keeton, Adam B.,Hartmann, Rolf W.,Engel, Matthias,Piazza, Gary A.,Abadi, Ashraf H.
supporting information, p. 4462 - 4477 (2021/05/04)
A ligand-based approach involving systematic modifications of a trisubstituted pyrazoline scaffold derived from the COX2 inhibitor, celecoxib, was used to develop novel PDE5 inhibitors. Novel pyrazolines were identified with potent PDE5 inhibitory activit
A simple iron-catalyst for alkenylation of ketones using primary alcohols
Sk, Motahar,Kumar, Ashish,Das, Jagadish,Banerjee, Debasis
, (2020/04/10)
Herein, we developed a simple iron-catalyzed system for the α-alkenylation of ketones using primary alcohols. Such acceptor-less dehydrogenative coupling (ADC) of alcohols resulted in the synthesis of a series of important α,β-unsaturated functionalized ketones, having aryl, heteroaryl, alkyl, nitro, nitrile and trifluoro-methyl, as well as halogen moieties, with excellent yields and selectivity. Initial mechanistic studies, including deuterium labeling experiments, determination of rate and order of the reaction, and quantitative determination of H2 gas, were performed. The overall transformations produce water and dihydrogen as byproducts.