14378-09-7Relevant academic research and scientific papers
Knoevenagel condensation in heterogeneous phase catalyzed by IR radiation and Tonsil Actisil FF
Obrador, Esteban,Castro, Martin,Tamariz, Joaquin,Zepeda, Gerardo,Miranda, Rene,Delgado, Francisco
, p. 4649 - 4663 (1998)
Infrared radiation promoted the synthesis of benzylidenemalononitriles, benzylidenecyanoacetamides and benzylidenecyanoacetic acids by condensation of aromatic aldehydes with the corresponding active methylene compound in the presence of Tonsil Actisil FF, without solvent. Mass of catalyst, solvent, and reaction time were assessed in order to improve the efficiency of this process.
Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases
Nitsche, Christoph,Steuer, Christian,Klein, Christian D.
experimental part, p. 7318 - 7337 (2012/01/05)
The 3-aryl-2-cyanoacrylamide scaffold was designed as core pharmacophore for inhibitors of the Dengue and West Nile virus serine proteases (NS2B-NS3). A total of 86 analogs was prepared to study the structure-activity relationships in detail. Thereby, it turned out that the electron density of the aryl moiety and the central double bond have a crucial influence on the activity of the compounds, whereas the influence of substituents of the amide residue is less relevant. The para-hydroxy substituted analog was found to be the most potent inhibitor in this series with a Ki-value of 35.7 μM at the Dengue and 44.6 μM at the West Nile virus protease. The aprotinin competition assay demonstrates a direct interaction of the inhibitor molecule with active centre of the Dengue virus protease. The target selectivity was studied in a counterscreen with thrombin and found to be 2.8:1 in favor of DEN protease and 2.3:1 in favor of WNV protease, respectively.
Pathways for the solvent-free condensation between schiff bases and methylenic compounds
Razus, Alexandra C.,Nitu, Carmen,Tecuceanu, Victorita,Birzan, Liviu
, p. 729 - 736 (2007/10/03)
Pathways for the solvent-free condensation between Schiff Bases and methylenic compounds are discussed taking into account the reported mechanistic purposes and new experimental data.
Tyrphostins I: Synthesis and Biological Activity of Protein Tyrosine Kinase Inhibitors
Gazit, Aviv,Yaish, Pnina,Gilon, Chaim,Levitzki, Alexander
, p. 2344 - 2352 (2007/10/02)
A novel class of low molecular weight proteine kinase inhibitors is described.These compounds consitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain.These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor.The potent EGF receptor kinase blockers examined were found to competitively inhibit the homologous insulin receptor kinase at 102-103 higher inhibitor concentrations in spite of the significant homology between these protein tyrosine kinases.These results demonstrate the ability to synthesize selective tyrosine kinase inhibitors.The most potent EGF receptor kinase inhibitors also inhibit the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on EGF independent cell growth.These results demonstrate the potential use of protein tyrosine kinase inhibitors as selective antiproliferative agents for proliferative diseases caused by the hyperactivity of protein tyrosine kinases.We have suggested the name "tyrphostins" for this class of antiproliferative compounds which act as protein tyrosine kinase blockers.
Head-to-Tail Assemblies of Dipolar, Piperazine-Linked Chromophores: Synthesis, X-ray Structure, and Dielectric Characterization
Katz, H. E.,Schilling, M. L.
, p. 7554 - 7557 (2007/10/02)
A dimer and a mixture of oligomers of acceptor-substituted anilines were prepared, either by Knoevenagel condensation of substituted cyanoacetylpiperazines with p-aminobenzaldehydes or by carbonyldiimidazole-promoted coupling of phenylpiperazines with p-a
Transmiision of substituent effects through extended systems II. Substituted cis and trans cinnamonitriles
Butt, G.,Topsom, R. D.
, p. 301 - 306 (2007/10/02)
Infrared data and 13C chemical shifts are reported for a series of p-substituted cis and m-substituted trans cinnamonitriles.The i.r. values include intensities for the benzene, ethylene and cyanide vibrations which allow an estimation of resonance effect
