50705-97-0Relevant articles and documents
GPR139 RECEPTOR MODULATORS
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Page/Page column 137; 139, (2021/06/26)
Compounds are provided that modulate the GPR139 receptor, compositions containing the same, and to methods of their preparation and use for treatment of a malcondition wherein modulation of the GPR139 receptor is medically indicated or beneficial. Such compounds have the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein R1, R4, R5, R9, R10, Q6, Q7, and Q12 are as defined herein.
METHOD OF SYNTHESIZING 1,2,4-TRIAZOLE-3-THIONE COMPOUNDS AND INTERMEDIATES THEREOF
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Paragraph 0051-0053, (2019/05/15)
Disclosed is a method of synthesizing 1,2,4-triazole-3-thione compounds and intermediates thereof. The method includes reacting a hydrazine with glyoxylic acid to form a hydrazono acetic acid intermediate followed by reacting the latter with thiocyanate to obtain the 1,2,4-triazole-3-thione compound. The raw materials involved in the present method are readily available, and the reaction is very specific in terms of regioselectivity, resulting in minimum by-product and high product yield. There are neither specific requirements for special equipment nor special operations such as high vacuum, high temperature, anhydrous and oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production.
Exceptionally rapid oxime and hydrazone formation promoted by catalytic amine buffers with low toxicity
Larsen, Dennis,Kietrys, Anna M.,Clark, Spencer A.,Park, Hyun Shin,Ekebergh, Andreas,Kool, Eric T.
, p. 5252 - 5259 (2018/06/21)
Hydrazone and oxime bond formation between α-nucleophiles (e.g. hydrazines, alkoxy-amines) and carbonyl compounds (aldehydes and ketones) is convenient and is widely applied in multiple fields of research. While the reactants are simple, a substantial drawback is the relatively slow reaction at neutral pH. Here we describe a novel molecular strategy for accelerating these reactions, using bifunctional buffer compounds that not only control pH but also catalyze the reaction. The buffers can be employed at pH 5-9 (5-50 mM) and accelerate reactions by several orders of magnitude, yielding second-order rate constants of >10 M-1 s-1. Effective bifunctional amines include 2-(aminomethyl)imidazoles and N,N-dimethylethylenediamine. Unlike previous diaminobenzene catalysts, the new buffer amines are found to have low toxicity to human cells, and can be used to promote reactions in cellular applications.
Design, synthesis and biological activity of novel substituted pyrazole amide derivatives targeting EcR/USP receptor
Deng, Xi-Le,Xie, Jin,Li, Yong-Qiang,Yuan, De-Kai,Hu, Xue-Ping,Zhang, Li,Wang, Qing-Min,Chi, Ming,Yang, Xin-Ling
supporting information, p. 566 - 570 (2016/04/26)
In order to discover highly active ecdysone analogs, a series of new substituted pyrazole amide derivatives were obtained using structure-guided optimization method and further screened for their insecticidal activities, in the basis of the core structures of the two active compounds N-(3-methoxyphenyl)-3-(tert-butyl)-1-phenyl-1H-pyrazole-5-carboxamide (6e) and N-(4-(tert-butyl)phenyl)-3-(tert-butyl)-1-phenyl-1H-pyrazole-5-carboxamide (6i), previously presented by us. The chemical structures of the title compounds were identified by spectral analyses. The preliminary bioassay results indicated that one among the synthesized pyrazole derivatives, compound 34, endowed with good activity against Mythimna Separata at 10 mg/L, which was equal to that displayed by the positive control tebufenozide. In addition, examples of molecular docking and molecular dynamics studies demonstrated that 34 may be the potential inhibitor to EcR and its docking conformation was similar to that of tebufenozide. In addition, increasing the hydrophobic effect and considering the suitable bulk effect on pyrazole ring are beneficial to the inhibiting activity to EcR and activity in vivo.
HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF
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Paragraph 00162, (2014/10/15)
Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
Quantification and mass isotopomer profiling of α-keto acids in central carbon metabolism
Zimmermann, Michael,Sauer, Uwe,Zamboni, Nicola
, p. 3232 - 3238 (2014/04/03)
Mass spectrometry has been established as a powerful and versatile technique for studying cellular metabolism. Applications range from profiling of metabolites to accurate quantification and tracing of stable isotopes through the biochemical reaction netw
First synthesis of a bromonitrilimine. Direct formation of 3- bromopyrazole derivatives
Foti, Francesco,Grassi, Giovanni,Risitano, Francesco
, p. 2605 - 2606 (2007/10/03)
The first example of the preparation of bromonitrilimine 3 is described. This precursor provides a convenient entry to a highly regioselective synthesis of 3-bromopyrazole derivatives 4 and 5.
A CONVENIENT SYNTHESIS OF 1-ARYL-Δ2-1,2,4-TRIAZOLIN-5-ONES FROM ARYLHYDRAZINES
Lyga, John W.
, p. 163 - 168 (2007/10/02)
1-Aryl-1,2,4-triazolin-5-ones are prepared from arylhydrazones of α-keto acids by treatment with diphenylphosphoryl azide.
