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2009 Vol VII #1


Acetylcholine and ethylene: do they share similar receptors and biological action?

B.A. Kurchii

Institute of Plant Physiology and Genetics, NAS of Ukraine
31/17 Vasylkivska Str., Kyiv, 03022, Ukraine

Summary: From chemical point of view acetylcholine (ACh) is a quaternary ammonium salt whose biological importance is connected with its role as a neurotransmitter between neurones and other neurocellular junctions. Earlier we have postulated (Kurchii, 1998) and then confirmed (Kurchii, Kurchii, 2000) that ACh under influence of physiological solution and alkaline mixture was decomposed with releasing of ethylene. Unfortunately using gas chromatograph we could not detected another two peaks on the chromatogram (Kurchii, Kurchii, 2000). Here we identified one of two unknown peaks: it is ethylene oxide. We have revealed that ethylene oxide was released in the quantity much more than ethylene during 10-20 min of decomposition in air or in drop of physiological solution. We have concluded that biological effects of ACh can be caused by action of ethylene oxide that is a very reactive agent and this is a prompt effect for short distance. Ethylene can migrate on the long distance and cause slow effects, but it should be preliminary activated because under normal conditions (temperature and pressure) it is a very inert chemical and cannot react with any substance. Nevertheless, it can be in vivo activated in the free radical addition reactions. Also as follows from our results the question about specific receptors for ACh is questionable.

Keywords:
acetylcholine, ethylene, ethylene oxide, free radicals, receptors.

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Synthesis and selectivity of 1-methoxycarbonylmethyl-3-arylamino-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-ones binding for CNS benzodiazepine receptors

N.A. Burenkova, V.I. Pavlovsky, I.A. Oleinich, I.A. Boyko, S.Yu. Makan, A.G. Artemenko, V.E. Kuzmin

A.V. Bogatsky Physico-Chemical Institute of the NAS of Ukraine
86 Lustdorfska doroga, Odesa, 65080, Ukraine

Abstract: Earlier, the methoxycarbonylmethyl fragment at the 1-position and the nitrophenylamine fragment at the 3-position of the 1,4-benzodiazepine ring, on the base of the QSAR analysis of series of 1,4-benzodiazepin-2-one derivatives [1], have been shown to gave compounds with increased affinity for peripheral benzodiazepine receptors (PBR). The 3-arylamine derivatives of 1-methoxycarbonylmethyl-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one were proposed for the directed synthesis as a promising high selective ligands of PBR. The target compounds were synthesized through the condensation of 1-methoxycarbonylmethyl-3-chloro-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one with substituted anilines. Affinities of synthesized compounds for the CNS benzodiazepine receptors of peripheral (PBR) and central (CBR) types were determined by the radioligand method in vitro. Selective PBR ligand with a high affinity 1-methoxycarbonylmethyl-3-(2'-nitro)phenylamino-7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepin-2-one, 7 (MX-1785, Ki(PBR)=19.1 nM, Ki(CBR)>10000 nM) was found among the studied compounds.

Keywords: 1,3-substituted 1,2-dihydro-3H-1,4-benzodiazepin-2-ones, affinity, benzodiazepine receptors, selectivity, QSAR analysis.

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Microwave assisted synthesis of pyrimido[4,5-d]pyrimidine derivatives in dry media

A.H. Kategaonkar, S.A. Sadaphal, K.F. Shelke, B.B. Shingate, M.S. Shingare

Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University
Aurangabad (M.S.) 431004, India

Summary: Pyrimido[4,5-d]pyrimidine derivatives were synthesized by using an efficient, facile and solvent-free procedure. Here, a non-conventional synthetic procedure has been developed where solid support of alumina is used as energy transfer medium under microwave irradiation (MWI) which devoids hazards of solution phase reactions. The reaction time has been brought down from minutes to seconds with improved yield as compared to reported method.

Keywords: solvent-free, alumina, barbituric acid, pyrimido[4,5-d]pyrimidines, microwave irradiation.

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2,6-Dinitroanilines: synthesis, herbicidal and antiprotozoan properties

.M. Britsun1, .. Yemets2, M.. Lozinskii1, Ya.B. Blume2

1 Institute of Organic Chemistry, NS of Ukraine
5 Murmanska Str., Kyiv, 02094, Ukraine

2 Institute of Food Biotechnology and Genomics, NS of Ukraine
2a Osipovskogo Str., Kyiv, 04123, Ukraine

Summary: The methods of dinitroanilines synthesis have been considered and summarized. There is described that 2,6-dinitroanilines are effective herbicides and anti-protozoan drugs. The mode of their action, toxicity, metabolism and methods of identification in the environment are discussed. It is considered the weak point of 2,6-dinitroanilines, namely their cytotoxicity, that can be reduced to desirable parameters by design and modification of chemical structures. It is shown also that studies on increasing the herbicidal and anti-protozoan activities as well as decreasing the cytotoxicity of dinitroanilines are continued now.

Keywords: 2,6-dinitroanilines, synthesis, herbicides, antiprotozoan activity.

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The synthesis of n-tret-butylcalix[4]arene with 14C-acetic acid residues

O.A. Alyeksyeyeva, A.P. Lukyanenko, N.V. Shneider, M.Ya. Golovenko

A.V. Bogatsky Physico-Chemical Institute of the NAS of Ukraine
86 Lustdorfska doroga, Odesa, 65080, Ukraine

Summary: 5,11,17,23-tetra-tert-butyl-25,27-bis[(14-methylcarbonylamido)etoxy]-26,28-dihydroxycalix[4]aren containing the 14C radioactive label was synthesized. For this compound the structure (using IR-, 1H NMR spectroscopy and mass-spectrometry), radiochromatographic purity (95 %) and given radioactivity were determined.

Keywords: 14-acetic acid modified calix[4]aren.

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Molecular complexes of the triterpene glycoside α-hederine with aliphatic proteinogenous amino acids

L.A. Yakovishin, M.A. Rubinson

Sevastopol National Technical University
33 University Str., Sevastopol, 99053, Ukraine

Summary: For the first time molecular complexes of the triterpene glycoside α-hederine (3-O-α-L-rhamnopyranosyl-(1→2)-O-α-L-arabinopyranoside of hederagenin) with aliphatic proteinogenous amino acids (glycine, L-alanine and L-valine) are received. The complex's formation is confirmed by IR-spectroscopy. omparative study of influence of α-hederine and its complexes on seeds germination Avena sativa L. has been made.

Keywords: 14-acetic acid modified calix[4]aren.

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This article is sponsored by Otava, Ltd.

The synthesis of 2-phenylisothiazolidine-3-one dioxide derivatives as inhibitors of protein kinase CK2

M.O. Chekanov, .R. Synyugin, S.S. Lukashov, S.M. Yarmoluk

Institute of Molecular Biology and Genetics, NAS of Ukraine
150 Zabolotnogo Str., Kyiv, 03143, Ukraine

Summary: Several 2-phenylisothiazolidine-3-one dioxide derivatives were synthesized and their in vitro activity against protein kinase CK2 was measured. The most active compound N-(3-acetylphenyl)-2-chloro-4-(4-methyl-1,1-dioxido-3-phenylisothiazolidin-2-yl) benzamide showed IC50 value 20 mM.

Keywords: 2-phenylisothiazolidine-3-one-1,1-dioxide, protein kinase CK2, inhibitor.

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This article is sponsored by Otava, Ltd.

Amino-3-arylindazole as template for Ser/Thr and Tyr kinase inhibitors revealing

S.S. Lukashov

Institute of Molecular Biology and Genetics, NAS of Ukraine
150 Zabolotnogo Str., Kyiv, 03143, Ukraine

Summary: 3-Arylindazole-amine derivatives activity against Ser/Thr and Tyr protein kinases is considered. Possibility and directions of 3-arylindazole-amines modification in course of revealing of new active derivatives are discussed.

Keywords: protein kinase, inhibitor, 3-arylindazole.

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This article is sponsored by Otava, Ltd.

Search for FGFR1 inhibitors among chromone derivatives

.. Grischenko, V.G. Bdzhola, O.P. Kukharenko, S.M. Yarmoluk

Institute of Molecular Biology and Genetics, NAS of Ukraine
150 Zabolotnogo Str., Kyiv, 03143, Ukraine

Summary: Proteinkinase FGFR1 plays a key role in angiogenesis regulation and tumor proliferation. Inhibitors of this kinase can be used for effective treatment of solid tumors and proliferative diseases. FGFR1 inhibitors searching were performed among 3500 chromone derivatives by virtual screening and in vitro testing. 6 compounds that inhibit kinase in micromolar range were detected from them. The most active compound was 2-(2-ethoxy-phenyl)-3-hydroxy-6-methyl-chromen-4-one (IC50 3.6 μM). Structure-activity relationship of tested compounds was investigated and binding model was proposed for flavonol inhibitors with FGFR1 ATP-binding site.

Keywords: proteinkinase FGFR1, flavonol, virtual screening.

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Dynamics of sodium counterions in the DNA ion-hydrate shell

O.M. Alekseyev, L.A. Bulavin, D.O. Shamayko

Kyiv National Taras Shevchenko University
1 Glushkova Ave, Kyiv, 03022, Ukraine

Summary: The lifetime of DNA counterions was determined using the phenomenological model, developed in this work. The counterions bonded to DNA are characterized by the lifetime and do not make contribution to the conductivity of the system. Free counterions, moving around the double helix make the main contribution to the conductivity. Using the theory of electrolyte conductivity, the formula connecting the counterion lifetime and conductivity was obtained. The conductivity of DNA aqueous solutions was determined for different concentrations of DNA (0.001-0.2 % by mass) at frequencies 0,1-100 kHz. The results show that in dilute DNA aqueous solutions (0.001 %) the lifetime is about 1 ms, and in the concentrated aqueous solutions (0.15 %) it is about 1 ms.

Keywords: DNA macromolecule, counterion, conductivity.

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