scholarly journals Study of the Biological Activity of Alkyl Derivatives of Tetrahydroisoquinolines

2021 ◽  
pp. 238-246
Author(s):  
Umida Khamidova ◽  
Ekaterina Terenteva ◽  
Mukaddas Umarova ◽  
Jaloliddin Abdurakhmanov ◽  
Sabirdjan Sasmakov ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Cancer Cells ◽  
Cytotoxic Effect ◽  
Normal Cells ◽  
Alkyl Derivatives ◽  
Antifungal Effects ◽  
Low Toxicity ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

A row of 1-alkyne (C6-C17) derivatives against tetrahydroisoquinoline have been synthesized. 1-alkyne (C6-C17) derivatives cytotoxicity against three lines of cancer cells and two lines of normal cells was studied. It was found that 1-tridecyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline exhibits a high cytotoxic effect with low toxicity to healthy cells. Antimicrobial activity of 1-alkyne (C6-C17) derivatives against 5 strains of bacteria and fungus was studied. It has been found that 1-nonyl-6,7-dimethoxy-1,3,4-tetrahydroisoquinoline exhibits strong antibacterial and antifungal effects.

scholarly journals N-Alkyl derivatives of diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside; synthesis and antimicrobial activity

2015 ◽  
Vol 11 ◽  
pp. 869-874 ◽  
Author(s):  
Agata Walczewska ◽  
Daria Grzywacz ◽  
Dorota Bednarczyk ◽  
Małgorzata Dawgul ◽  
Andrzej Nowacki ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Fungi ◽  
Pharmacological Properties ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside is a synthetic saponin exhibiting attractive pharmacological properties. Different pathways tested by us to obtain this glycoside are summarized here. Moreover, the synthesis of N-alkyl and N,N-dialkyl derivatives of the glucopyranoside is presented. Evaluation of antibacterial and antifungal activities of these derivatives indicates that they have no inhibitory activity against Gram-negative bacteria, whereas many of the tested N-alkyl saponins were found to inhibit the growth of Gram-positive bacteria and human pathogenic fungi.

scholarly journals Alkylamino and aralkylamino derivatives of avarone and its mimetic as selective agents against non-small cell lung cancer cells, their antibacterial and antifungal potential

2018 ◽  
Vol 83 (11) ◽  
pp. 1193-1207 ◽  
Author(s):  
Marko Jeremic ◽  
Jelena Dinic ◽  
Milica Pesic ◽  
Marija Stepanovic ◽  
Irena Novakovic ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cancer Cells ◽  
Small Cell Lung Carcinoma ◽  
Multidrug Resistant ◽  
Small Cell ◽  
Small Cell Lung ◽  
Cell Lung Carcinoma ◽  
Normal Keratinocytes ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

In this paper, the synthesis of fourteen alkylamino and arylamino derivatives of sesquiterpene quinone avarone and its model compound tert-butylquinone is described. Branched, cyclic, allylic and benzylic alkylamino/arylamino groups were introduced into the quinone moiety. For all the obtained derivatives, their biological activity and redox properties were studied. The cytotoxic activity of the synthesized derivatives towards multidrug resistant (MDR) human non-small cell lung carcinoma NCI-H460/R cells, their sensitive counterpart NCI-H460 and human normal keratinocytes (HaCaT) was investigated. The antimicrobial activity towards Gram-positive and Gram-negative bacteria, and fungal cultures was determined. Some of the synthesized derivatives showed selectivity for cancer cells, including MDR cells. Regarding their cell death induction potential, the most promising compounds were allylamino derivatives, preferentially triggering apoptosis, with high selectivity for cancer cells, including MDR cells. Several compounds showed promising antimicrobial activity, comparable to those of commercial antibiotic and antimycotic agents.

scholarly journals SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF NOVEL BISPIDINE DERIVATIVES

2021 ◽  
pp. 69-74
Author(s):  
AIGUL YE. MALMAKOVA ◽  
VALENTINA K. YU ◽  
KALDYBAY D. PRALIYEV ◽  
ALTYNAI B. KALDYBAYEVA ◽  
MARZHAN K. AMIRKULOVA
Keyword(s):  
Biological Activity ◽  
Local Anesthetic ◽  
The Novel ◽  
Anesthetic Activity ◽  
Local Anesthetic Activity ◽  
Scientific Representations ◽  
Depth Study ◽  
Low Toxicity ◽  
Pharmacological Screening ◽  
Derivatives Of

Objective: Derivatives of 3,7-diazabicyclo[3.3.1]nonan-9-one attract considerable attention from pharmacists for the treatment of a wide rangeof diseases. According to this interest, the novel derivatives of 3-cyclopropanmethyl-7-alkoxyalkyl-3,7-diazabicyclo[3.3.1]nonan-9-one withisopropoxypropyl and ethoxypropyl substituents in the position 7 had been synthesized to study their biological activity and toxicity. The practicalsignificance of the work is in the accumulation and development of scientific representations about diazabicyclic compounds, methods for theirsynthesis, structure, and properties, which can subsequently be used in a targeted design and identification of even more complex systems, as wellas in the development of further research in the field of 3,7-diazabicyclo[3.3.1]nonanes. For this purpose, complexes of the synthesized compoundswith β-cyclodextrin are obtained and their biological activity is investigated at the Department of Pharmacology of S.D. Asfendiyarov Kazakh NationalMedical University with the aid of the pharmacological tests.Methods: An experimental study of local anesthetic activity on the models of infiltration, conduction anesthesia, and acute toxicity of synthesizedmolecules was carried out using primary screening methods.Results: As a result of pharmacological screening, it has been found that the compounds exhibit local anesthetic activity and low toxicity and wasrecommended for in-depth study of their pharmacological properties.Conclusion: It turned out that a nature of the N-alkoxyalkyl radical does not affect the toxicity of cyclopropanmethyl- substituted bispidines. In theseries of O-benzoyloximes of bispidinones, the isopropoxypropyl- substituted analog is 1.3 times less toxic than ethoxypropyl- one.

scholarly journals Synthesis of alkyl derivatives of 3,7,10-trioxo-2,4,6,8,9,11-hexaaza[3.3.3]propellane and evaluation of their biological activity

2021 ◽  
Vol 101 (1) ◽  
pp. 19-26
Author(s):  
А.А. Sinitsyna ◽  
◽  
S.G. Il’yasov ◽  
Keyword(s):  
Biological Activity ◽  
Influenza A ◽  
Bacillus Pumilus ◽  
Maximum Yield ◽  
Methyl Derivative ◽  
Tert Butyl ◽  
Alkyl Derivatives ◽  
Derivatives Of ◽  
And Staphylococcus Aureus ◽  
Moderate Yield

Today 3,7,10-trioxo-2,4,6,8,9,11-hexaaaza[3.3.3]propellane (THAP) has not yet received widespread re-search attention due to the complexity of the synthesis. This work is devoted to the development of a method for the THAP derivatives synthesis, as well as to the study of their biological activity in comparison with al-kyl-substituted glycolurils (subject of comparison). ТНАРwas N-alkylated to furnish novel hexaalkyl deriva-tives of ТНАРwith methyl, ethyl and propyl substituents. The conditionsfor obtaining the maximum yield of the target productwere optimizedon the base of methyl derivative. The reaction proceeded in DMSO/КОНat 75–80ºC for 13hours in a moderate yield of 56%. The ethyl and propyl derivatives of ТНАРwere synthe-sized under the same conditions. The biological activity of the obtained ТНАРalkyl derivatives and glycoluril alkyl derivatives was evaluated against Sporosarcina ureae, Bacillus pumilus, Salmonella typhimurium and Staphylococcus aureus bacteria and influenza A virus. All the samples were found to exhib-it antibacterial activity against Staphylococcus aureus.It was shown that 2,4,6,8,9,11-hexapropyl-ТНАР, di-tert-butyl-diphenyl-, di-tert-butyl-dibenzyl-, di-tert-butyl-dimethyl-and di-isopropyl-dibenzylglycoluril, have exhibited also toxicity to living cells besides antiviral activity

scholarly journals Overview on the Side Effects of Doxorubicin

2020 ◽  
Author(s):  
Chittipolu Ajaykumar
Keyword(s):  
Side Effects ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Cell Apoptosis ◽  
Cytotoxic Effect ◽  
Molecular Mechanisms ◽  
Current Understanding ◽  
Preventive Strategies ◽  
Normal Cells ◽  
Dna Strand

Doxorubicin is an anthracycline antibiotic extracted from the bacterium Streptomyces peucetius. Its cytotoxic effect produced by intercalating with DNA causing breakdown of DNA strand which causes cancer cell apoptosis. Despite being an effective anticancer agent it causes several crucial side effects like carditoxicity, neuropathy, hepatotoxicity, nephrotoxicity, alopecia, typhlitis, myelosuppression, neutropenia, anaemia, thrombocytopenia, nausea, and diarrhoea were caused mainly due to the inability to distinguish between cancer cells and normal cells. This chapter mainly focuses on doxorubicin’s side effects, current understanding of the molecular mechanisms, and management and preventive strategies of doxorubicin’s cardiotoxicity during the treatment of various type of cancer.

Influence of chlorine and methyl substituents and their position on the antimicrobial activities and crystal structures of 4-methyl-1,6-diphenylpyrimidine-2(1H)-selenone derivatives

2021 ◽  
Vol 77 (10) ◽  
Author(s):  
Izabela Korona-Głowniak ◽  
Wojciech Nitek ◽  
Waldemar Tejchman ◽  
Ewa Żesławska
Keyword(s):  
Crystal Structure ◽  
Biological Activity ◽  
Intermolecular Interactions ◽  
Current Knowledge ◽  
Antimicrobial Activities ◽  
Mutual Orientation ◽  
Antibacterial And Antifungal Activities ◽  
Chlorine Substituent ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Derivatives of 4-methyl-1,6-diphenylpyrimidine-2(1H)-selenone show very strong antimicrobial activity. In order to extend the current knowledge about the features responsible for the biological activity, crystal structure analyses are presented for 4-methyl-1-(2-methylphenyl)-6-phenylpyrimidine-2(1H)-selenone (1), 4-methyl-1-(3-methylphenyl)-6-phenylpyrimidine-2(1H)-selenone (2), 4-methyl-1-(4-methylphenyl)-6-phenylpyrimidine-2(1H)-selenone (3) (all C18H16N2Se) and 1-(4-chlorophenyl)-4-methyl-6-phenylpyrimidine-2(1H)-selenone (4) (C17H13ClN2Se). Furthermore, the antibacterial and antifungal activities of these compounds were evaluated. All the presented derivatives crystallize in the space group P21/c with one molecule in the asymmetric unit. The molecular geometries differ slightly in the mutual orientation of the rings. The packing of molecules in the crystals is dominated by C—H...N and C—H...Se intermolecular interactions. Additionally, in the crystal structure of 4, C—H...Cl intermolecular interactions are observed. The introduction of a methyl or chlorine substituent improves the biological activity, while its position significantly affects biological activity only in case of the chlorine substituent.

scholarly journals Antibacterial and antifungal effects of alcoholic extracts of 41 medicinal plants growing in Turkey

2010 ◽  
Vol 28 (No. 1) ◽  
pp. 53-60 ◽  
Author(s):  
Ö. Ertürk
Keyword(s):  
Antimicrobial Activity ◽  
Alnus Glutinosa ◽  
Viscum Album ◽  
Antibacterial And Antifungal Activities ◽  
Galega Officinalis ◽  
Ethanolic Extracts ◽  
Thymus Capitatus ◽  
Antifungal Effects ◽  
Rhus Coriaria ◽  
Antibacterial And Antifungal

The antibacterial and antifungal activities of crude ethanolic extracts of 41 traditional medicinal plant species belonging to 26 families were tested against four bacteria and two fungi: <I>Bacillus subtilis, Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans</I>, and <I>Aspergillus niger</I>. Of the 41 plants tested, 39 showed antimicrobial activity against one or more species of microorganisms. While the crude extracts from <I>Nigellea arvensis</I> did not show antimicrobial activity against the test microorganisms, <I>Pistasia lentiscus</I> showed only antifungal activity against A. <I>niger</I>. The most active antimicrobial plants were <I>Cuminum cyminum, Jasminium officinale, Thymus capitatus, Viscum album, Tanecetum sorbifolium, Pimpinella anisum, Galega officinalis, Liguidamber orientalis, Rhus coriaria, Alnus glutinosa, Pimental officinalis, Achillea coarctata</I>, and <I>Cameli sinensis</I>.

Synthesis, Molecular Characterization, and Biological Activity of Novel Synthetic Derivatives of Chromen-4-one in Human Cancer Cells

2006 ◽  
Vol 49 (13) ◽  
pp. 3800-3808 ◽  
Author(s):  
Vivek Barve ◽  
Fakhara Ahmed ◽  
Shreelekha Adsule ◽  
Sanjeev Banerjee ◽  
Sudhir Kulkarni ◽  
...  
Keyword(s):  
Biological Activity ◽  
Cancer Cells ◽  
Molecular Characterization ◽  
Human Cancer ◽  
Human Cancer Cells ◽  
Synthetic Derivatives ◽  
Derivatives Of

scholarly journals Preparation and Antimicrobial Properties of Alginate and Serum Albumin/Glutaraldehyde Hydrogels Impregnated with Silver(I) Ions

Chemistry ◽  
2021 ◽  
Vol 3 (2) ◽  
pp. 672-686
Author(s):  
Louise Gallagher ◽  
Alanna Smith ◽  
Kevin Kavanagh ◽  
Michael Devereux ◽  
John Colleran ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Serum Albumin ◽  
Calcium Alginate ◽  
Metal Ion ◽  
Antimicrobial Properties ◽  
Hydrogel Beads ◽  
Composite Beads ◽  
Antifungal Effects ◽  
Propylene Glycol Alginate ◽  
Antibacterial And Antifungal

Calcium alginate (CaALG) hydrogel beads and two sets of composite beads, formed from a combination of calcium alginate/propylene glycol alginate/human serum albumin (CaALG/PGA/HSA) and from calcium alginate with the quaternary ammonium salt, (3-(trimethoxysilyl)propyl)-octadecyldimethylammonium chloride (QA), (CaALG/QA), were prepared. Bovine serum albumin (BSA) was condensed with glutaraldehyde (GLA) to form a BSA/GLA hydrogel. The corresponding Ag+-containing gels of all of the above hydrogels were also formed, and slow leaching of the biocidal transition metal ion from the gels bestowed broad spectrum antimicrobial activity. In the absence of added Ag+, CaALG/QA was the only material to deliver marginal to moderate antibacterial and antifungal effects. The Ag+ impregnated hydrogel systems have the potential to maintain the antimicrobial properties of silver, minimising the risk of toxicity, and act as reservoirs to afford ongoing sterility.

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