We report results of small-angle neutron scattering (SANS) measurements on aqueous solutions of 1,7-heptanediol in the molarity range 0.11–1.5 mol dm−3 at room temperature. The experimental data show aggregation of the diol molecules within the whole studied concentration range. The scattering ...
The mixed micellization behavior of surface active ionic liquids (SAILs), 1-dodecyl-3-methylimidazolium chloride, [C12mim][Cl], and 1-tetradecyl-3-methylimidazolium chloride, [C14mim][Cl] with an amphiphilic drug amitriptyline hydrochloride (AMT) have been studied using surface tension and condu...
The thermodynamics and interfacial behavior of the mixed micellization of a trisubstituted imidazolium based surface active ionic liquid (SAIL), 1-dodecyl-2,3-dimethylimidazolium chloride [C12bmim][Cl], with an antidepressant amphiphilic drug amitriptyline hydrochloride (AMT) have been studied b...
The first synthesis of actiketal (RK-441S), an antibiotic from Streptomyces pulveraceus subsp. epiderstagenes, was achieved from 5,7-dimethylbenzofuran and dimethyl glutaconate via palladium-assisted coupling reaction as a key step.
The reintroduction of thalidomide in the pharmacotherapy greatly stimulated the interest in the synthesis and pharmacological evaluation of phthalimide analogs with new and improved activities and also greater safety. In the present study, we evaluated the activities of two phthalimide analogs d...
A convenient method for the preparation of 4- or 5-substituted 3-sulfonyl-δ-lactams via regioselective reduction of N-alkyl-3-sulfonyl glutarimides is described. Formal synthesis of (±)-paroxetine and (±)-tacamonine is also reported.
Transmission electron microscopy (TEM) has been used to investigate the microdeformation mechanisms in thin films (
Molecular probes based on 3-[(dodecylthiocarbonyl)methyl]glutarimide (DTCM-glutarimide) were synthesized and assessed for inhibitory activity against LPS-induced NO production. Among the probes examined, several derivatives exhibited potential for use in determining the target proteins of DTCM-g...
The synthesis of various functionalized or spirobicyclic glutarimides by a novel tandem process has been disclosed. The reaction involves a base-catalyzed Michael addition of active methylene compounds to secondary conjugated amides, followed by intramolecular N-acylation of the carboxamido grou...
We describe an efficient route towards the synthesis of fused bicyclic glutarimides using facile [3+3] reaction of α-sulfonylacetamides with different α,β-unsaturated esters as the key step. Intramolecular cyclization of 4-substituted 3-sulfonylglutarimide to form 5,6-, 6,6- or 6,7-fused bicy...
We have isolated 9-methylstreptimidone from microorganism as a new NF-κB inhibitor. Later, we designed 3-[(dodecylthiocarbonyl) methyl]-glutarimide (DTCM-glutarimide) as an analog of this compound, which shows anti-inflammatory activity in vivo. In the present research, we found that DTCM-gluta...
By the method of 1H NMR prescreening and tracing the diagnostic signals, 6-methylpyridinone derivatives, (8R,9S)-dihydroisoflavipucine (1), (8S,9S)-dihydroisoflavipucine (2), 3-(1-hydroxy-4-methyl-2-oxopentylidene)-6-methylpyridine-2,4(1H,3H)-dione (3), 4-hydroxy-3-(2-hydroxy-4-methylpentanoyl)-...
The molecular structure of 4-methylpiridine-N-oxide, 4-MePyO, has been studied by gas-phase electron diffraction monitored by mass spectrometry (GED/MS) and quantum chemical (DFT) calculations. Both, quantum chemistry and GED analyses resulted in CS molecular symmetry with the planar pyridine ri...
Verticillium sp. GF39, catalyzing the oxidation of 1-methylisoquinoline to 1-methylisoquinoline N-oxide, was found to be the highest N-oxide producer. Under the optimized reaction conditions, the whole cells of Verticillium sp. GF39 formed 5 mM 1-methylisoquinoline N-oxide from 1-methylisoquinol...
The review is concerned with three Na+-dependent biotin-containing decarboxylases, which catalyse the substitution of CO2 by H+ with retention of configuration (ΔG°′=−30 kJ/mol): oxaloacetate decarboxylase from enterobacteria, methylmalonyl-CoA decarboxylase from Veillonella parvula and Propi...
Theoretical calculations have been carried on four compounds, bicyclo[4.1.0]heptan-7-one cis and trans, 2-cyclohepten-1-one and cycloheptenyl cation to determine their UV, IR and NMR spectra (chemical shifts). In the case of the known 2-cyclohepten-1-one the agreement is satisfactory. Predictive...
The synthesis and photochemistry of 4,4-diphenyl-2-cyclohepten-1-one are reported. Despite the presence of phenyls at C-4, irradiation of the title compound affords only the [2+2] cycloaddition products; no phenyl-migration products normally associated with 4,4-diphenyl-2-cyclohexe-1-one photoch...
A new synthetic pathway to the final compound 1-[(1S)-5’,11’-dihydrospiro[cyclopentane-1,10’-dibenzo[a,d]cyclohepten]-3-yl]-3-azetidinecarboxylic acid (1) was set up. The two preparative chiral HPLC separations needed in the first route were successfully avoided and replaced by two diastereom...
Reaction off non-enolizable 2-n-butylthiomethylene cyclohexanones with methoxy (phenylthio)methyllithium, followed by hydrolysis off the diastereomeric mixture off resulting alcohols, provides a new and efficient ring enlargement reaction for the synthesis of the previously unreported 3-formyl-2...
In this study, an unprecedented [4 + 3] annulation of aza-ortho-quinone methides with azomethine imines was achieved under mild conditions. Annulation via the aza-Michael/aminalization sequence served as a useful method to synthesize biological heterocycles in good-to-excellent yields.
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