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1.
Molecules ; 25(23)2020 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-33271872

RESUMO

The design of new dual-function inhibitors simultaneously preventing hydrate formation and corrosion is a relevant issue for the oil and gas industry. The structure-property relationship for a promising class of hybrid inhibitors based on waterborne polyurethanes (WPU) was studied in this work. Variation of diethanolamines differing in the size and branching of N-substituents (methyl, n-butyl, and tert-butyl), as well as the amount of these groups, allowed the structure of polymer molecules to be preset during their synthesis. To assess the hydrate and corrosion inhibition efficiency of developed reagents pressurized rocking cells, electrochemistry and weight-loss techniques were used. A distinct effect of these variables altering the hydrophobicity of obtained compounds on their target properties was revealed. Polymers with increased content of diethanolamine fragments with n- or tert-butyl as N-substituent (WPU-6 and WPU-7, respectively) worked as dual-function inhibitors, showing nearly the same efficiency as commercial ones at low concentration (0.25 wt%), with the branched one (tert-butyl; WPU-7) turning out to be more effective as a corrosion inhibitor. Commercial kinetic hydrate inhibitor Luvicap 55 W and corrosion inhibitor Armohib CI-28 were taken as reference samples. Preliminary study reveals that WPU-6 and WPU-7 polyurethanes as well as Luvicap 55 W are all poorly biodegradable compounds; BODt/CODcr (ratio of Biochemical oxygen demand and Chemical oxygen demand) value is 0.234 and 0.294 for WPU-6 and WPU-7, respectively, compared to 0.251 for commercial kinetic hydrate inhibitor Luvicap 55 W. Since the obtained polyurethanes have a bifunctional effect and operate at low enough concentrations, their employment is expected to reduce both operating costs and environmental impact.


Assuntos
Materiais Biocompatíveis/química , Gases/química , Interações Hidrofóbicas e Hidrofílicas , Poliuretanos/química , Água/química , Corrosão , Reologia
2.
Neurosci Lett ; 706: 110-113, 2019 07 27.
Artigo em Inglês | MEDLINE | ID: mdl-31078677

RESUMO

Two novel pyrimidine derivatives, RG2 and RG6, were studied using a rat's model of peripheral nerve injury. Toe-spreading reflex and skin sensitivity to pinch in the foot were monitored to follow recovery of motor and sensory functions in the treated animals. The remyelation rate in the distal segment of the damaged nerve was also studied using morphological analysis of cross-sections of the nerve stained with methylene blue. The obtained data demonstrate a high stimulating effect of RG2 and RG6 on the restoration of motor and sensory functions of the sciatic nerve, as well as on the post-traumatic regeneration of myelin fibers. Possible mechanisms of the observed effects are discussed.


Assuntos
Regeneração Nervosa/efeitos dos fármacos , Traumatismos dos Nervos Periféricos/tratamento farmacológico , Pirimidinas/farmacologia , Nervo Isquiático/efeitos dos fármacos , Animais , Masculino , Compressão Nervosa , Pirimidinas/uso terapêutico , Ratos , Recuperação de Função Fisiológica/efeitos dos fármacos , Nervo Isquiático/lesões
3.
Curr Org Synth ; 16(1): 160-164, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31965930

RESUMO

AIM AND OBJECTIVE: Some ferrocenyl derivatives are active in vitro and in vivo against cancer. Generally, ferrocenyl derivatives for cancer research have three key components: a ferrocene moiety, a conjugated linker that lowers the oxidation potential and some derivative (peptide, nucleobase and others) that can interact with biomolecules. Since the pyrimidine fragment can easily pass through the membrane into the cells and become involved in metabolism; it appears to be promising. Furthermore, this fragment is an electron-acceptor group, so a spacer can be excluded. Therefore, the synthesis of 6-ferrocenylpyrimidin-4(3H)-one derivatives and the study of their anticancer activity have scientific and practical interest. METHODS: The syntheses of 6-ferrocenylpyrimidin-4(3H)-one derivatives were performed by the condensation of ethyl 3-ferrocenyl-3-oxopropionate with thiourea or acetamidine or guanidine. The cytotoxicity of four 6- ferrocenylpyrimidin-4(3H)-one derivatives was evaluated by using the MTT assay in vitro against Human breast adenocarcinoma MCF-7 and normal human skin fibroblast HSF cells. The tested derivatives induced a concentration-dependent cytotoxic response in cell lines. RESULTS: A study of the cytotoxic activity of 6-ferrocenylpyrimidin-4(3H)-one derivatives by the MTT test has found that all compounds have a dose-dependent toxic effect on the lines of breast cancer cells (MCF-7) and normal human fibroblast cells (HSF). The most pronounced cytotoxic effect is exhibited by 2-methyl-6-ferrocenylpyrimidin- 4(3H)-one (MCF-7, IC50 17 ± 1 µM). CONCLUSION: The experimental results confirm the importance of investigation and design of ferrocenylpyrimidin- 4(3H)-one derivatives as anticancer agents. Compounds where the pyrimidine derivatives are directly linked to the ferrocene unit rather than via a spacer group also may be of interest for antiproliferative drug design.


Assuntos
Antineoplásicos/farmacologia , Compostos Ferrosos/farmacologia , Pirimidinonas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/toxicidade , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Compostos Ferrosos/síntese química , Compostos Ferrosos/toxicidade , Fibroblastos/efeitos dos fármacos , Humanos , Células MCF-7 , Pirimidinonas/síntese química , Pirimidinonas/toxicidade
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