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Ethyl Derivative (ethyl + derivative)

Distribution by Scientific Domains

Chemistry	100%

Selected Abstracts

Synthesis and Pharmacological Evaluation of N -(Dimethylamino)ethyl Derivatives of Benzo- and Pyridopyridazinones

ARCHIV DER PHARMAZIE, Issue 1 2009
Wanda Pakulska
Abstract New N -(dimethylamino)ethyl derivatives of phthalazinones and pyridopyridazinones 7, 9 were synthesized and assayed as potential analgesic agents in the hot-plate, tail-flick, and writhing tests. Pharmacological assay demonstrated that eight (in ten) of the newly synthesized compounds showed antinociceptive activity. Especially, 2-[2-(dimethylamino)ethyl]-4-phenyl-2H -phthalazin-1-one 7a showed remarkably higher antinociceptive activity in all tests. This is connected with influence on supraspinal, spinal, and peripheral structures. The decreased sensitivity to the pain stimulus in the hot-plate was higher than that of metamizole. [source]

The Hammett equation applied to the nucleophilic displacement of ions and ion pairs on substituted benzenesulphonates

JOURNAL OF PHYSICAL ORGANIC CHEMISTRY, Issue 5 2001
Sergio Alunni
Abstract Nucleophilic substitution on meta - and para -substituted methyl benzenesulphonates was studied with two chloride salts with different structures: NBu4Cl or KCl-Kryptofix 2,2,2. Treating the results with the Acree equation shows that the reaction proceeds by two reaction paths, one involving the chloride ion and the other, slower one, involving the ion pairs. Treating the results with the Hammett equation gives consistent data, and shows that , is positive and nearly the same for the two reaction paths (,,,,+2). The reactivity of methyl p -nitrobenzenesulphonate was compared with that of the corresponding ethyl derivative, and it is shown that the methyl derivative reacts faster than the ethyl derivative in both paths. The results are interpreted based on the assumption that in both paths a negative charge is developed on the leaving group in the transition state, and that the activated complex is linear. Copyright © 2001 John Wiley and Sons, Ltd. [source]

Synthesis, Structural Evaluation, and Estrogen Receptor Interaction of 4, 5-Bis(4-hydroxyphenyl)imidazoles

ARCHIV DER PHARMAZIE, Issue 10 2002
Ronald Gust
Abstract 4, 5-Bis(4-hydroxyphenyl)imidazoles with 2, 2,-H (1), 2, 2,-F (2), 2, 2,-Cl (3), and 2, 2,6-Cl (4) substituents in the aromatic rings were synthesized by oxidation of the respective methoxy-substituted (R, S)/(S, R)-4, 5-diaryl-2-imidazolines with MnO2 and subsequent ether cleavage with BBr3. N -alkylation of 1 and 3 with ethyl iodide yielded the compounds 5 and 6. The imidazoles were characterized by NMR spectroscopy and tested for estrogen receptor binding in a competition experiment with [3H]estradiol using calf uterine cytosol. Gene activation was verified in a luciferase assay using estrogen receptor positive MCF-7-2a cells stably transfected with the plasmid EREwtcluc. All halide substituted imidazoles competed with estradiol for the binding site at the estrogen receptor. The N -ethyl derivative 6 showed the highest relative binding affinity of 1.26 %. Treatment of MCF-7-2a cells, however, did not lead to gene activation. The relative activation of 6 amounted only to 10 % at 1,M compared to E2 (100 %). [source]

2-Amino-5-methyl-1,3,4-thiadiazole and 2-amino-5-ethyl-1,3,4-thiadiazole

ACTA CRYSTALLOGRAPHICA SECTION C, Issue 10 2001
Daniel E. Lynch
The structures of 2-amino-5-methyl-1,3,4-thiadiazole, C3H5N3S, and 2-amino-5-ethyl-1,3,4-thiadiazole, C4H7N3S, have been determined for comparison with unsubstituted 2-amino-1,3,4-thiadiazole. Despite their different space groups (P21/n and Pbca, respectively), the packing modes of the methyl and ethyl derivatives are similar, with comparable three-dimensional hydrogen-bonding associations. This is in contrast to the hydrogen-bonding network in 2-amino-1,3,4-thiadiazole, which is one-dimensional and has denser packing. It is shown that both packing forms are different polymorphs of a specific subunit of each array. [source]