Lyudmila Sidorenko

• National University of Pharmacy

The aim. Technological process validation of manufacturing medical devices is a necessary condition for confirming the ability to continuously produce high-quality medical devices, reduce or eliminate the number of defects, improve the level of product quality, and is also one of the main requirements for product certification on the European Union...

The aim. To study the behaviour of enisamium iodide, thiloron dihydrochloride, morpholinium thiazotate, and the suitability of the previously developed GC-FID methodology in soil. Materials and methods. The determination of the Enisamium iodide, Tilorone dihydrochloride, and Morpholinium thiazotate in soil gas chromatography with a flame ionization...

The aim: implementation of the principles of green chemistry by regenerating the synthesis solvent 1,2,4-trichlorobenzene and reusing it during the synthesis of the Naphazoline nitrate substance. Study of the influence of the regenerated solvent on the quality of the final product by controlling analytical quality parameters. Development of a metho...

Pharmaceutical companies in Ukraine aspire to develop their innovative medicinal products and successfully introduce them to the global market. However, along with the prospects of increased usage of these pharmaceuticals, there arises a challenge of heightened waste production, making them a part of the over twenty million tons of PPCPs produced a...

Fluoroquinolones have been studied for more than half a century. Since the 1960s, four generations of these synthetic antibiotics have been created and successfully introduced into clinical practice. However, they are still of interest for medicinal chemistry due to the wide possibilities for chemical modification, with subsequent useful changes in...

The current situation in medicine and pharmacy still requires the time and effort of medicinal chemists, who must develop new synthetic approaches and create promising molecules that can turn into novel antimicrobials. Due to the problem of resistance to well-known antibiotics combined with the occurrence of new diseases that we observe, we can be...

A method for the determination of amizone and amixin in the same sample and in their mixture with antibiotics (ceftriaxone, tetracycline, ampicillin and levofloxacin) was developed using reversed-phase highperformance liquid chromatography equipped with a photodiode array detector. A SunFire C18 column, a mobile phase consisting of sodium perchlora...

One of the main steps in the pharmaceutical development of drugs is the choice of quality control methods. The correctness of the method must be confirmed by validation. In addition, manufacturers take into account various economic and environmental factors. It is especially important to determine the above aspects for domestic and promising drugs,...

Based on the interpretation of regulatory requirements to describe the approach to risk-oriented medical devices design and development strategy and approaches to their certification in Ukraine market. The approach to the medical devices design and development strategy is described taking into account the classification by level of risk; a tree of...

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesiz...

The aim of the work. Among all the representatives of four generations of fluoroquinolones ciprofloxacin (CIPRO) and norfloxacin (NOR) remain widely used and prescribed antibiotics in clinical practice. However, the problem of resistance towards them is gradually increasing. Thus, our investigation is dedicated to chemical modification of C-7 posit...

Crocus sativus L. is one of the world’s most famous saffron production crops and its enormous by-products, such as leaves, are an excellent source of bioactive compounds with potential nutritional applications. The total phenolic content of Crocus leaves was 5.44 ± 0.01 mg GAE/g, and the total flavonoid content was 2.63 ± 0.05 mg RE/g, respectively...

In order to identify new regularities of the “structure–analgesic activity” relationship in the series of 2,1-benzothiazine derivatives, the synthesis of methyl 4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxylate and a group of its analogs substituted in the benzene moiety of the molecule, as well as their mono-and diammonium salts, was perfor...

In order to study polymorphic modifications of N-(4-trifluoromethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamide, which is of interest as a promising analgesic, its three colorless crystal forms with different habitus have been obtained: sticks of ethyl acetate, plates of meta-xylene and blocks of ortho-xylene. However, the X-ray...

The title mol­ecule crystallizes as a di­methyl­formamide monosolvate, C19H14N2O6S2·C3H7NO. The mol­ecule was expected to adopt mirror symmetry but slightly different conformational characteristics of the condensed benzo­thia­zine ring lead to point group symmetry 1. In the crystal, mol­ecules form two types of stacking dimers with distances of 3.4...

According to our quantum and chemical calculations 4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxylic acid imidazolide is theoretically almost as reactive as its 2-carbonyl analog, and it forms the corresponding N-pyridyl-4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamides with many aminopyridines. However, in practice, the sulfo group int...

6-Hy­droxy-N-(4-meth­oxy­phen­yl)-4-oxo-2,4-di­hydro-1H-pyrrolo­[3,2,1-ij]quinoline-5-carboxamide, C19H16N2O4, possesses strong diuretic properties and can be used as a new hypertension remedy. Two polymorphic modifications of this compound have been found, namely the triclinic polymorph (space group P), with one mol­ecule in the asymmetric unit, a...

In accordance with the principles of “me-too” technique, the preparative method for obtaining has been proposed, and the synthesis of a large series of new N-(arylalkyl)-6-hydroxy-2-methyl-4-oxo-2,4-dihydro-1H-pyrrolo[3,2,1-ij]quinoline-5-carboxamides as structurally close analogs of tricyclic pyrrolo- and pyridoquinoline diuretics has been carried...

Continuing the search for new potential analgesics among the derivatives of 4-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxylic acid, the possibility of obtaining its esters by the alkylation of the corresponding sodium salt with iodoethane in dimethyl sulfoxide (DMSO) at room temperature was studied. It was found that under such conditions, tog...

Continuing a targeted search for new leading structures with diuretic action among tricyclic derivatives of hydroxyquinolines, which are of interest as potential inhibitors of aldosterone synthase, the synthesis of a series of the corresponding pyrido[3,2,1-ij]quinoline-6-carboxanilides was carried out by amidation of ethyl-7-hydroxy-5-oxo-2,3-dihy...

As potential newanalgesics, the corresponding 4-hydroxy-2,2-dioxo-1H-2λ⁶,1-benzothiazine- 3-carboxanilides have been obtained by amidation of ethyl 4-hydroxy-2,2-dioxo-1H-2λ⁶, 1-benzothiazine-3-carboxylate with aniline and its halogenated analogsin boiling dry xylene. The peculiarities of the mass and nuclear magnetic resonance (¹H and¹³C) spectra...

Being guided by the methodological principles of "chiral switches", the synthesis of S- and R-enantiomers of 1-allyl-4-hydroxy-6,7-dimethoxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid (1-ethylpyrrolidin-2-ylmethyl)-amide hydrochloride has been carried out. According to the results of the biological research, it has been found that the ability of...

We have carried out the synthesis and a comparative analysis of the acidic properties of a large group of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids. Features of the recorded NMR spectra of these compounds are discussed together with their analgesic properties. Keywords4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids-pKa-analgesic activity...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Bromination of N-allyl-substituted 4-hydroxy-2-quinolinones with molecular bromine in acetic acid or carbon tetrachloride occurs with closing of a five membered oxazole ring to give 2-bromomethyl-5-oxo-1,2-dihydro-5H-oxazolo[3,2-a]quinoline.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

The spatial structural features of 3-bromo-3-ethoxycarbonyl-2,4-dioxo-1,2,3,4-tetrahydroquinolines have been studied by X-ray analysis. It has been experimentally confirmed that these compounds can be regarded as potential brominating agents.

The reaction of 2-ethoxycarbonylmethyl-4H-3,1-benzoxazin-4-one with malononitrile in dry pyridine leads to 1-hydroxy-3,6-dioxo-4,6-dihydro-3H-pyrimido[1,2-a]quinoline-5-carbonitrile. Acetoacetic and cyanoacetic esters under analogous conditions form anilides of 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid while diethyl malonate gives N,N′...

1-R-4-Hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid anilides have been prepared. It has been shown experimentally that these compounds are brominated by molecular bromine in glacial acetic acid at position 4 of the anilide fragment. The antitubercular properties of the compounds synthesized are discussed.

The alkylation of the ethyl esters of 4-methyl, 4-chloro-, and 4-amino substituted 2-oxo-1,2-dihydroquinoline-3-carboxylic acid by ethyl iodide in the system DMF/K2CO3 has been studied. Features of the structure of the starting compounds and their effect on the ratio of the N-and O-alkyl products formed are discussed.

The optimal conditions for obtaining hetarylamides of 4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxylic acid are suggested on the basis of derivatographic investigations. The 1H NMR spectra of the synthesized compounds, their spatial structure, and also the results of a study of their antitubercular properties are discussed.

Alkaline hydrolysis of the ethyl ester of 4-(cyanoethoxycarbonylmethyl)-2-oxo-1,2-dihydroquinoline-3-carboxylic acid is accompanied by decarboxylation with loss of two molecules of CO2 and leads to 4-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid.

The title compound, C14H13NO5, exhibits a resonance-assisted hydrogen bond O—H⋯O=C [2.505 (4) Å], which leads to a lengthening of the carbonyl C=O bond, a shortening of the C—OH bond and delocalization of the electron density within the dihydro­pyridine ring.

The title compound, C14H13NO5, exhibits a resonance-assisted hydrogen bond O—H⋯O=C [2.505 (4) Å], which leads to a lengthening of the carbonyl C=O bond, a shortening of the C—OH bond and delocalization of the electron density within the dihydro­pyridine ring.

X-ray diffraction study of the title compound, C11H11NO2, (I), has shown that the molecular geometry is similar to that of 1-ethyl-4-hydroxy-2-oxo-1,2-di­hydro­quinoline-3-carboxyl­ic acid, (II) [Shishkina, Shishkin, Ukrainets, Dakkah & Sidorenko (2002). Acta Cryst. E58, o254–o256]. Observed elongations of the bonds around the N atom are caused by...

Export Date: 15 June 2012, Source: Scopus, doi: 10.1023/B:JORY.0000048891.01018.36, Language of Original Document: English, Correspondence Address: STC Institute of Single Crystals, NAS, Ukraine, Kharkovemail: shishkin@xray.isc.kharkov.com, References: Ukrainetz, V., Gorokhova, O.V., Tarans, S.G., (1994) Khim. Geterotsikl. Soedin., pp. 1211-1213;

In the structure of the title compound, C11H10N2O3, pairs of mol­ecules are linked into centrosymmetric dimers by N—H⋯O hydrogen bonds, which involve the cyclo­amino N—H and the keto C=O groups. In addition, the 4-amino group is involved in both intramolecular and intermolecular hydrogen bonds.

An X-ray diffraction study of the title compound, C12H11NO4, has shown that this compound exists in the crystal as the 2-oxo-4-hydroxy tautomer. The formation of two O—H⋯O=C-type intramolecular hydrogen bonds leads to the elongation of both exocyclic and carboxyl­ic C=O double bonds involved in the hydrogen bonding, causes shortening of the exocycl...

The synthesis, antitubercular, anti-HIV, and antitumor activity of the 4-(adamant-1-yl)thiazolyl-2-amides of 1-R-4-hydroxy-2-oxoquinoline-3-carboxylic acids have been studied. An efficient method for purifying the 4-hydroxy-2-oxoquinoline derivatives from their metal salts is proposed.

The reaction product of 4-chloro-2-oxo-1,2-di­hydro­quinoline-3-carboxyl­ic acid with p-phenetidine is 4-(4-ethoxy­phenyl­amino)-2-oxo-1,2-di­hydro­quinoline, C17H16N2O2. The mol­ecules form centrosymmetric hydrogen-bonded dimers.

In the title compound, C24H30N2O3·0.5C3H8O, the formation of intramolecular O—H⋯O and N—H⋯O hydrogen bonds causes considerable changes in the bond lengths within the amido­pyridine fragment. This fact probably results in the unusual reactivity of the ether group in this type of compound.

A preparative method is proposed for obtaining N-substituted 1H-4-hydroxy-2-oxoquinoline-3-acetic acid amides. X-Ray diffraction analysis of one of the synthesized compounds has been carried out. The effect of the obtained substances on thyroid gland function has been studied.