Perm State Pharmaceutical Academy

Perm’, Russia

Perm State Pharmaceutical Academy

Perm’, Russia

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Ivshina I.B.,Russian Academy of Sciences | Vikhareva E.V.,Perm State Pharmaceutical Academy | Richkova M.I.,Russian Academy of Sciences | Mukhutdinova A.N.,Russian Academy of Sciences | Karpenko J.N.,Perm State Pharmaceutical Academy
World Journal of Microbiology and Biotechnology | Year: 2012

Drotaverine [1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline] hydrochloride, an antispasmodic drug derived from benzylisoquinoline was evaluated for its biodegradability using a bacterial strain Rhodococcus rhodochrous IEGM 608. The experiments were performed under aerobic conditions with rhodococci cultures able to degrade drotaverine. In the presence of glucose, the removal efficiency of drotaverine by free Rhodoccocus cells pre-grown with isoquinoline was above 80 % (200 mg/l, initial concentration) after 25 days. Rhodococcus immobilization on hydrophobized sawdust enhanced the biodegradation process, with the most marked drotaverine loss being observed during the first 5 days of fermentation. High metabolic activity of rhodococcal cells towards drotaverine was confirmed respirometrically. GC-MS analysis of transformation products resulting from drotaverine biodegradation revealed 3,4-diethoxybenzoic acid, 3,4-diethoxybenzaldehyde and 3,4-diethoxybenzoic acid ethyl ester which were detected in the culture medium until drotaverine completely disappeared. Based on these major and other minor metabolites, putative pathways for drotaverine biodegradation were proposed. The obtained data broadened the spectrum of organic xenobiotics oxidized by Rhodoccocus bacteria and proved their potential in decontamination of natural ecosystems from pharma pollutants. © 2012 Springer Science+Business Media B.V.


Kalinin D.V.,Perm State Pharmaceutical Academy | Kalinina S.A.,Perm State Pharmaceutical Academy | Dolzhenko A.V.,University of Selangor | Dolzhenko A.V.,Curtin University Australia
Heterocycles | Year: 2013

The amino substituted triazine ring was annelated to aminoazoles using a new effective synthetic procedure. The method of preparation involved initial formation of azolylformamidines in the reaction of aminoazoles with N,N-dimethylformamide dimethyl acetal followed by the triazine ring closure with cyanamide affording therefore fused aminotriazines. © 2013 The Japan Institute of Heterocyclic Chemistry.


Gein V.L.,Perm State Pharmaceutical Academy | Mar'Yasov M.A.,Perm State Pharmaceutical Academy
Russian Journal of Organic Chemistry | Year: 2015

Three-component condensation of methyl 4-(furan-2-yl)- and 4-(thiophen-2-yl)-2,4-dioxobutanoates with aromatic aldehydes and 1,3-thiazol-2-amine afforded 5-aryl-4-(hetaren-2-ylcarbonyl)-3-hydroxy-1-(1,3-thiazol-2-yl)-2,5-dihydro-1H-pyrrol-2-ones. Reactions of the latter with hydrazine and phenylhydrazine gave pyrrolo[3,4-c]pyrazol-6-ones and 3-phenylhydrazones, while the corresponding oximes were obtained in reactions with hydroxylamine. © 2015 Pleiades Publishing, Ltd.


Dolzhenko A.V.,University of Selangor | Dolzhenko A.V.,Curtin University Australia | Kalinina S.A.,Perm State Pharmaceutical Academy | Kalinin D.V.,Perm State Pharmaceutical Academy
RSC Advances | Year: 2013

A novel multicomponent strategy for the efficient synthesis of 5-aza-adenines was developed. 5-Aza-adenines were prepared in a one-pot fashion from 5-amino-1,2,4-triazoles, cyanamide and triethyl orthoformate under microwave irradiation. The operational simplicity, efficiency and accessibility of this method make it highly attractive for the generation of bioactive compound libraries. © 2013 The Royal Society of Chemistry.


Kalinina S.A.,Perm State Pharmaceutical Academy | Kalinin D.V.,Perm State Pharmaceutical Academy | Dolzhenko A.V.,Sunway University | Dolzhenko A.V.,Curtin University Australia
Tetrahedron Letters | Year: 2013

A new, efficient, catalyst-free, one-pot, three-component method for the synthesis of 2-amino-substituted 7-amino-1,2,4-triazolo[1,5-a][1,3,5]triazines using 3,5-diamino-1,2,4-triazoles, cyanamide, and triethyl orthoformate is developed. The reaction proceeds smoothly under microwave-assisted heating. Advantages of the method include using easily available reagents, short reaction times, and operational simplicity. © 2013 Elsevier Ltd. All rights reserved.


Korkotian E.,Weizmann Institute of Science | Bombela T.,Perm State Pharmaceutical Academy | Odegova T.,Perm State Pharmaceutical Academy | Zubov P.,Perm State Pharmaceutical Academy | Segal M.,Weizmann Institute of Science
PLoS ONE | Year: 2013

The effects of ethanol on neuronal network activity were studied in dissociated cultures of rat hippocampus. Exposure to low (0.25-0.5%) ethanol concentrations caused an increase in synchronized network spikes, and a decrease in the duration of individual spikes. Ethanol also caused an increase in rate of miniature spontaneous excitatory postsynaptic currents. Higher concentrations of ethanol eliminated network spikes. These effects were reversible upon wash. The effects of the high, but not the low ethanol were blocked by the GABA antagonist bicuculline. The enhancing action of low ethanol was blocked by apamin, an SK potassium channel antagonist, and mimicked by 1-EBIO, an SK channel opener. It is proposed that in cultured hippocampal networks low concentration of ethanol is associated with SK channel activity, rather than the GABAergic receptor. © 2013 Korkotian et al.


Kalinin D.V.,Perm State Pharmaceutical Academy | Kalinina S.A.,Perm State Pharmaceutical Academy | Dolzhenko A.V.,Curtin University Australia
Heterocycles | Year: 2012

The triazine ring bearing a trichloromethyl group was annelated to various aminoazoles using a new effective synthetic procedure. The method of preparation involved initial formation of trichloroacetamidines in the reaction of aminoazoles with trichloroacetonitrile followed by the triazine ring closure with triethyl orthoformate affording therefore the titled compounds. © 2012 The Japan Institute of Heterocyclic Chemistry.


Korkotian E.,Weizmann Institute of Science | Botalova A.,Perm State Pharmaceutical Academy | Odegova T.,Perm State Pharmaceutical Academy | Segal M.,Weizmann Institute of Science
NeuroToxicology | Year: 2015

The effects of chronic exposure to moderate concentrations of ethanol were studied in cultured hippocampal neurons. Network activity, assessed by imaging of [Ca2+]i variations, was markedly suppressed following 5 days of exposure to 0.25-1% ethanol. The reduced activity was sustained following extensive washout of ethanol, but the activity recovered by blockade of inhibition with bicuculline. This reduction of network activity was associated with a reduction in rates of mEPSCs, but not in a change in inhibitory synaptic activity. Chronic exposure to ethanol caused a significant reduction in the density of mature dendritic spines, without an effect on dendritic length or arborization. These results indicate that chronic exposure to ethanol causes a reduction in excitatory network drive in hippocampal neurons adding another dimension to the chronic effects of alcohol abuse. © 2015 Elsevier Inc.


Gein V.L.,Perm State Pharmaceutical Academy | Bobrovskaya O.V.,Perm State Pharmaceutical Academy | Sitnikova A.A.,Perm State Pharmaceutical Academy
Russian Journal of General Chemistry | Year: 2014

Methyl aroylpyruvates react with sodium 4-aminobenzenesulfonylacetamide in acetic acid to afford 4-aryl-2-hydroxy-4-oxo-2-butenoic acids N-(4-acetylaminosulfonylphenyl)amides. The latter were studied in reactions with hydrazine hydrate. © 2014 Pleiades Publishing, Ltd.


Molokhova E.I.,Perm State Pharmaceutical Academy | Sorokina Yu.V.,Perm State Pharmaceutical Academy
Antibiotiki i Khimioterapiya | Year: 2015

Rheological properties of mild pharmaceutical formulations (creams) with glucocorticosteroids, such as Triderm (Belgium), Akriderm GK (Russia) and Kanizon plus (India) were studied. The study revealed differences in the structural-strength properties of the medicines (viscosity, critical shear stress). The necessity of rheological investigations during development of generic medicines was shown.

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