InterBioScreen Ltd.

Chernogolovka, Russia

InterBioScreen Ltd.

Chernogolovka, Russia
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Zubenko A.A.,Federal State Budgetary Scientific Institution North Caucasus Zonal Scientific Research Veterinary Institute | Kartsev V.G.,InterBioScreen Ltd. | Morkovnik A.S.,Southern Federal University | Divaeva L.N.,Southern Federal University | And 4 more authors.
Tetrahedron Letters | Year: 2017

A novel one-pot synthetic route to the poorly studied 4-heteroaryl-1,2-dihydro-3-benzazepine motif from 3,4-dihydroisoquinolinium compounds is described. The synthetic approach is based on heterocyclic ring expansion of isoquinoline substrates upon reaction with chloromethyl-substituted heterocycles. The scope and limitations of the reaction were investigated to give a series of novel heteroaryl-3-benzazepines. © 2017 Elsevier Ltd


Osterman I.A.,Moscow State University | Khabibullina N.F.,University of Illinois at Chicago | Komarova E.S.,Moscow State University | Kasatsky P.,RAS Petersburg Nuclear Physics Institute | And 6 more authors.
Nucleic Acids Research | Year: 2017

The emergence ofmulti-drug resistant bacteria is limiting the effectiveness of commonly used antibiotics, which spurs a renewed interest in revisiting older and poorly studied drugs. Streptogramins A is a class of protein synthesis inhibitors that target the peptidyl transferase center (PTC) on the large subunit of the ribosome. In this work, we have revealed the mode of action of the PTC inhibitor madumycin II, an alanine-containing streptogramin A antibiotic, in the context of a functional 70S ribosome containing tRNA substrates. Madumycin II inhibits the ribosome prior to the first cycle of peptide bond formation. It allows binding of the tRNAs to the ribosomal A and P sites, but prevents correct positioning of their CCA-ends into the PTC thus making peptide bond formation impossible. We also revealed a previously unseen drug-induced rearrangement of nucleotides U2506 and U2585 of the 23S rRNA resulting in the formation of the U2506·G2583 wobble pair that was attributed to a catalytically inactive state of the PTC. The structural and biochemical data reported here expand our knowledge on the fundamental mechanisms by which peptidyl transferase inhibitors modulate the catalytic activity of the ribosome. © The Author(s) 2017.


Zubenko A.A.,North Caucasian Zonal Scientific Research Veterinary Institute | Divaeva L.N.,RAS Institute of Chemistry | Morkovnik A.S.,RAS Institute of Chemistry | Kartsev V.G.,InterBioScreen Ltd | And 6 more authors.
Russian Journal of Bioorganic Chemistry | Year: 2017

9-Bromocotarnine in the stable perchlorate form has been obtained by the interaction of cotarnine with bromine. The reaction of 9-bromocotarnine with α-haloketones is accompanied by the extension of the six-membered hetero-ring to seven-membered ring and led to previously unknown 4-acyl-9-bromo-3-methyl-6-methoxy-7,8-methylendioxy-1,2-dihydro-3-benzazepines. Some of these compounds have been shown to have only moderate antibacterial (against Staphylococcus aureus, Escherichia coli) and fungistatic (Penicillium italicum) activities, but none of them has been shown to have a pronounced protistocidal activity against Colpoda steinii. © 2017, Pleiades Publishing, Ltd.


Suzdalev K.F.,Southern Federal University | Babakova M.N.,Southern Federal University | Kartsev V.G.,InterBioScreen Ltd. | Krasnov K.A.,Institute of Toxicology FMBA of Russia
Heterocycles | Year: 2015

New indolin-2-one derivatives, containing in its molecules eight-membered pseudo-cycle with unusually short intramolecular hydrogen bond in OHO-bridge have been synthesized by reaction of 2-chloro-1-alkyl-1H-indole-3-carbaldehyde with barbituric acids or 5-methyl-2-phenyl-2,4-dihydropyrazol-3-one. Under the action of amines they undergo fragmentation to 5-aminomethylenebarbituric acids or 4-aminomethylenepyrazolones and 1-alkyl-1,3-dihydroindol-2-ones. © 2015 The Japan Institute of Heterocyclic Chemistry


Krasnov K.A.,Federal Medical Biological Agency | Kartsev V.G.,InterBioScreen Ltd. | Khrustalev V.N.,RAS Nesmeyanov Institute of Organoelement Compounds
Tetrahedron | Year: 2010

Knoevenagel products formed by the condensation of N-monoalkyl barbituric acids with o-tert-amino benzaldehydes undergo tert-amino effect reactions (T-reactions) yielding 1-alkyl-2,4,6-trioxoperhydropyrimidine-5-spiro-3′- (1′,2′,3′,4′-tetrahydroquinoline) derivatives as a mixture of (S*,S*)- and (S*,R*)-diastereomers. Mostly, the major diastereomer has the S*,S*-configuration. According to X-ray diffraction data in the solid form and NOE data in solution, diastereoselectivity of the T-reactions can be associated with the structure of the Knoevenagel products whose conformation is fixed by the strong intramolecular C-H⋯π interaction. © 2010 Elsevier Ltd. All rights reserved.


Khalymbadzha I.A.,Ural Federal University | Chupakhin O.N.,Ural Federal University | Fatykhov R.F.,Ural Federal University | Charushin V.N.,Ural Federal University | And 2 more authors.
Synlett | Year: 2016

A new method for the direct metal-free C–H functionalization of electron-deficient triazines with fragments of naturally occurring and synthetic 5,7-dihydroxycoumarins is reported. It has been found that the reaction of 5,7-dihydroxycoumarins with triazines proceeds under mild conditions, showing a high chemo- and regioselectivity. Copyright © 2016, Georg Thieme Verlag. All rights reserved.


Baranov D.S.,RAS Institute of Chemical Kinetics and Combustion | Ryabichev A.A.,RAS Institute of Chemical Kinetics and Combustion | Mamatyuk V.I.,RAS Institute of Organic Chemistry | Gatilov Y.V.,RAS Institute of Organic Chemistry | And 2 more authors.
Mendeleev Communications | Year: 2012

Reaction between 2-alkyl-4-arylbut-3-yn-2-ols and guanidine in refluxing pyridine affords 2-amino-5,5-dialkyl-4-arylmethylidene-2-oxazolines. © 2012 Mendeleev Communications. All rights reserved.


Sirakanyan S.N.,Armenian National Academy of Sciences | Kartsev V.G.,InterBioScreen Ltd. | Hovakimyan A.A.,Armenian National Academy of Sciences | Noravyan A.S.,Armenian National Academy of Sciences | Shakhatuni A.A.,Armenian National Academy of Sciences
Chemistry of Heterocyclic Compounds | Year: 2013

A method has been developed for the synthesis of new 8-amino-substituted 5-propyl(isobutyl)-1,2,3,4-tetra-hydropyrimido[4',5':4,5]furo[2,3-c] isoquinolines from 3-oxo derivatives of 5,6,7,8-tetra-hydroisoquinolines. Isomeric triazoles, condensed at the edge [c] of the pyrimidine ring, have been obtained from the 8-hydrazino derivatives. A Dimroth rearrangement was carried out in acidic medium. © 2013 Springer Science+Business Media New York.


Kartsev V.G.,InterBioScreen Ltd | Zubenko A.A.,North Caucasian Zonal Research Veterinary Institute | Morkovnik A.S.,Southern Federal University | Divaeva L.N.,Southern Federal University
Tetrahedron Letters | Year: 2015

A new, one-pot approach to 4-acyl-1,2-dihydro-3-benzazepines has been proposed proceeding via a six- to seven-membered heterocyclic ring expansion under the action of α-haloketones. © 2015 Elsevier Ltd. All rights reserved.

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