- Synthesis and Anticholinesterase Activity Evaluation of Asymmetric Azines
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Azines or di-imines are compounds containing R1R2C=N-N=CR3R4 fragment in its structure. These compounds have received special attention due to their importance as intermediates in the synthesis of drugs and substances with diverse pharmacological activities. In this research, twelve compounds derived of asymmetric azines of aryl aldehydes and aryl ketones were synthesized by microwave assisted irradiation, and their ability to inhibit acetylcholinesterase (AChE) enzyme was tested using the Ellman method. Among the evaluated azines, five compounds were able to inhibit AChE, especially compounds (7E, 8E)-1-benzylidene-2-(1-(4-nitrophenyl)ethylidene)hydrazine (7) and (7E,8E)-2-(1-(4-nitrophenyl)ethylidene)-1-((pyridin-2-yl)methylene)hydrazine (14), which showed percentage inhibition of 18.34% and 17.43% at concentrations of 22.46 and 10 μM, respectively.
- Figueredo, Andreza S.,Queiroz, Jaqueline E.,Dias, Lucas D.,Vidal, Hérika D. A.,Machado, Ingrid V.,Vila Verde, Giuliana M.,Aquino, Gilberto L. B.
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p. 544 - 549
(2019/11/20)
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- TRIPHENYLETHYLENE COMPOUNDS AND USES THEREOF
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Triphenylethylene compounds as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the des
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Paragraph 0147-0148
(2017/06/19)
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- A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β
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The design and synthesis of dual aromatase inhibitors/selective estrogen receptor modulators (AI/SERMs) is an attractive strategy for the discovery of new breast cancer therapeutic agents. Previous efforts led to the preparation of norendoxifen (4) deriva
- Zhao, Li-Ming,Jin, Hai-Shan,Liu, Jinzhong,Skaar, Todd C.,Ipe, Joseph,Lv, Wei,Flockhart, David A.,Cushman, Mark
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p. 5400 - 5409
(2016/10/24)
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- New synthetic approach to α-chlorocinnamates: First example of synthesis of functionally substituted alkenes using catalytic olefination reaction
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A new simple and efficient transformation of carbonyl compounds to α-chlorocinnamates is described. Catalytic olefination reaction with ethyl trichloroacetate gives target alkenes in moderate to good yields. The reaction with aromatic aldehydes proceeds stereoselectively to form preferably Z-isomers.
- Nenajdenko, Valentine G.,Lenkova, Olesya N.,Shastin, Alexey V.,Balenkova, Elizabeth S.
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p. 573 - 577
(2007/10/03)
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- A convenient method for the preparation of N-unsubstituted hydrazones of aromatic ketones and aldehydes
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A general and useful method for the synthesis of N-unsubstituted hydrazones of aromatic ketones and aldehydes in good yields was elaborated. The use of a large excess of hydrazine hydrate and catalytic amounts of p-toluenesulfonic acid makes it possible to prepare the hydrazones without an admixture of the corresponding azine.
- Shirinian,Belen'kii,Krayushkin
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p. 2171 - 2172
(2007/10/03)
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- Synthesis, characterisation, and phase behaviour of some azines with potential optical nonlinearities of second order
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Some azines with potential nonlinear optical properties of the second order have been synthesised by condensation of the appropriate hydrazones and aldehydes. The compounds have been chemically functionalised to allow their use in the synthesis of polymers containing the azine groups as side chain pendants. The characterisation of the phase behaviour, performed by DSC, X-ray diffraction and polarising microscopy methods, shows that most of the compounds exhibit enantiotropic liquid crystalline properties. Some peculiar features concerning solid state polymorphism have also been investigated.
- Centore,Panunzi,Roviello,Sirigu,Villano
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p. 107 - 120
(2007/10/03)
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