7699-03-8Relevant academic research and scientific papers
Structure-Based Design of High-Affinity Fluorescent Probes for the Neuropeptide Y Y1Receptor
Müller, Christoph,Gleixner, Jakob,Tahk, Maris-Johanna,Kopanchuk, Sergei,Laasfeld, T?nis,Weinhart, Michael,Schollmeyer, Dieter,Betschart, Martin U.,Lüdeke, Steffen,Koch, Pierre,Rinken, Ago,Keller, Max
, p. 4832 - 4853 (2022/03/27)
The recent crystallization of the neuropeptide Y Y1 receptor (Y1R) in complex with the argininamide-type Y1R selective antagonist UR-MK299 (2) opened up a new approach toward structure-based design of nonpeptidic Y1R ligands. We designed novel fluorescent probes showing excellent Y1R selectivity and, in contrast to previously described fluorescent Y1R ligands, considerably higher (~100-fold) binding affinity. This was achieved through the attachment of different fluorescent dyes to the diphenylacetyl moiety in 2 via an amine-functionalized linker. The fluorescent ligands exhibited picomolar Y1R binding affinities (pKi values of 9.36-9.95) and proved to be Y1R antagonists, as validated in a Fura-2 calcium assay. The versatile applicability of the probes as tool compounds was demonstrated by flow cytometry- and fluorescence anisotropy-based Y1R binding studies (saturation and competition binding and association and dissociation kinetics) as well as by widefield and total internal reflection fluorescence (TIRF) microscopy of live tumor cells, revealing that fluorescence was mainly localized at the plasma membrane.
Compound with alpha substituted phenyl structure as well as preparation method and sterilization agent thereof
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Paragraph 0067-0068, (2019/11/12)
The invention relates to the technical field of sterilization and disinfection materials and in particular to a compound with an alpha substituted phenyl structure as well as a preparation method anda sterilization agent thereof. The compound with the alpha substituted phenyl structure, which is provided by the invention, has a sterilization effect by promoting solidification and denaturation ofproteins of pathogenic microorganisms, particularly has a good killing effect on pathogenic bacteria such as escherichia coli, staphylococcus aureus, pseudomonas aeruginosa and bacillus subtilis variants, in addition has no corrosion function on metals, is free of irritant smell, good in water solubility and green and environment-friendly, can be used as an effective component of sterilization agents and are widely applied to various industries.
Synthesis of Malononitrile-Substituted Diarylmethines via 1,6-Addition of Masked Acyl Cyanides to para -Quinone Methides
Zhao, Kun,Zhi, Ying,Wang, Ai,Enders, Dieter
, p. 872 - 880 (2017/11/29)
An efficient method for the synthesis of malononitrile-substituted diarylmethines through 1,6-conjugate addition of para -quinone methides with masked acyl cyanide (MAC) reagents has been developed. Under mild conditions, the scalable reaction occurs in good to excellent yields providing a straightforward access to a series of malononitrile-substituted diarylmethines. The synthetic utility of this protocol has been demonstrated in the synthesis of bioactive compounds.
Highly site-selective direct C-H bond functionalization of phenols with α-aryl-α-diazoacetates and diazooxindoles via gold catalysis
Yu, Zhunzhun,Ma, Ben,Chen, Mingjin,Wu, Hai-Hong,Liu, Lu,Zhang, Junliang
supporting information, p. 6904 - 6907 (2014/06/09)
An unprecedented direct C-H bond functionalization of unprotected phenols with α-aryl α-diazoacetates and diazooxindoles was developed. A tris(2,4-di-tert-butylphenyl) phosphite derived gold complex promoted the highly chemoselective and site-selective C-H bond functionalization of phenols and N-acylanilines with gold-carbene generated from the decomposition of diazo compounds, furnishing the corresponding products in moderate to excellent yields at rt. The salient features of this reaction include readily available starting materials, unprecedented C-H functionalization rather than X-H insertion, good substrate scope, mild conditions, high efficiency, and ease in further transformation. To the best of our knowledge, this is the first example of C-H functionalization of unprotected phenols with diazo compounds.
