7514-02-5Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of compounds with a new scaffold as anti-neuroinflammatory agents for the treatment of Alzheimer's disease
Fang, Yuying,Xia, Wenjuan,Cheng, Bao,Hua, Pei,Zhou, Huihao,Gu, Qiong,Xu, Jun
, p. 129 - 138 (2018/03/06)
Twenty-eight compounds with a new scaffold were designed and synthesized by assembling fragments derived from known agents such as stilbenes and piperazinyl pyrimidines. Many strategies have been explored to improve the druggability of these series of compounds, such as increasing the distance between two benzene rings in the scaffold and introducing functional groups at designated positions. These compounds were validated for their anti-neuroinflammatory activity in BV2 cells. Experimental results reveal that the most active compound 8b can inhibit nitric oxide (NO), tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) production with IC50 values of 1.0, 2.6, and 0.5 μM, respectively. The compound can also significantly modulate the MAPK pathways through inhibiting the phosphorylation of JNK, ERK1/2, and p38 MAPK without disturbing NF-κB pathway. Parallel artificial membrane permeation assay demonstrated that the most active compound can overcome the blood-brain barrier (BBB). Therefore, this compound can be a promising lead for the treatment of Alzheimer's disease.
GUANIDINE DERIVATIVES AS TRPC MODULATORS
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Page/Page column 42-43, (2014/02/16)
The present invention is directed to guanidine derivatives as inhibitors of transient receptor potential canonical channels (TRPC channels), in particular TRPC3 and/or TRPC6 and/or TRPC7 activity, more particularly TRPC6 activity. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by TRPC channels (Formula (I))
Synthesis and biological evaluation of some stilbene derivatives
Karki, Subhas Somalingappa,Bhutle, Santosh Ramarao,Sahoo, Subhas,Reddy, Ratnakar,Balzarini, Jan,De Clercq, Erik,Darji, Satyanarayana Y.
experimental part, p. 1349 - 1356 (2012/05/05)
Several trans and cis stilbenes with substitution n the olefinic bridge were synthesized and characterized by IR, NMR and mass spectroscopy in an effort to obtain ubstances that could be more readily formulated. All the synthesized compounds were screened against Molt4/C8, CEM and L1210 cell lines. None of these compounds were ndowed with pronounced cytostatic activity. However,Schiff derivatives emerged as cytostatic agents (IC50: 0.77-10 μg/ml) that deserve further investigation. Springer Science+Business Media, LLC 2010.
Reactions of carbonyl compounds in basic solutions. Part 34. The mechanism of the base-catalysed ring fission of 2,3-diphenylcycloprop-2-en-1-one
Bowden, Keith,Burgess, Emma J.
, p. 1594 - 1600 (2007/10/03)
The rate coefficients for the base-catalysed ring fission of a series of 2-phenyl-3-(2-, 3-or 4-substituted phenyllcycloprop-2-en-1-ones to give the corresponding (E)-2,3-diphenylacrylic acids have heen determined in water at 30.0 °C, as well as for the unsubstituted compound at 40.0, 50.0 and 60.0 °C. The effects of meta-and para-substituents on the rates have been correlated using the Hammett equation to give a reaction constant, p, equal to ca 1.2 at 30 °C. For the unsubstituted compound, the activation parameters have been calculated and the kinetic solvent isotope effect has been studied. The effects of ortho-substituents on the rates appear to be mainly polar, rather than steric, in origin. The evidence indicates a mechanistic pathway which proceeds by addition of hydroxide anion to the ketone, which is rate-determining. The adduct suffers ring fission to give the final product via a carbanionic intermediate.
