scholarly journals THE STUDY OF THE ANTIMICROBIAL ACTIVITY OF SOME NEW AZO DERIVATIVES OF PYRIDOXINE AND THEIR ZINC COMPLEXES

2012 ◽  
Vol 17 (2) ◽  
pp. 60-62
Author(s):  
N. N. Aliyev ◽  
F. A. Heydarova
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Maximum Dose ◽  
Zinc Complexes ◽  
Low Toxicity ◽  
Azo Derivatives ◽  
First Time ◽  
Derivatives Of ◽  
Candia Albicans ◽  
Test Cultures

For the first time with the use of conventional techniques the overall toxicity and the antimicrobial activity of some new substances - pyridoxine azo derivatives (mercurions), obtained an international registration (CAS, USA) and their zinc-complexes have been studied. St. aureus, E.coli, Pseudomonas aeruginosa, and Candia albicans were used as a test cultures. The investigated compounds were established to have low toxicity (LD 50 failed to detect, with a maximum dose of introduced animals as 0.01 g ≈ 20 g), and some of them were shown to have pronounced antimicrobial activity. In contrast to free mercurions their zinc complexes show activity against strains of some microorganisms (St. aureus, Candida albicans), as well as similar antimicrobial activity in the lower (2-4 fold) concentrations.

scholarly journals Antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata

2020 ◽  
Vol 4 (1) ◽  
pp. 49
Author(s):  
Gracielle Oliveira Sabbag Cunha ◽  
Ana Paula Terezan ◽  
Andreia Pereira Matos ◽  
Marcela Carmen De Melo Burger ◽  
Paulo Cezar Vieira ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Methyl Esters ◽  
Carboxyl Group ◽  
Isomeric Mixture ◽  
E Coli ◽  
Bacillus Subtilis Atcc ◽  
Derivatives Of

This study evaluated the antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata (Melastomataceae) against five microorganisms: Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6623), Pseudomonas aeruginosa (ATCC 15442), and Candida albicans (ATCC 10231). The isomeric mixture of ursolic and oleanolic acids was active against S. aureus (MIC = 250 μg mL-1) and against E. coli, B. subtilis, and P. aeruginosa (MIC = 500 μg mL-1). The flavone 5,6,7-trihydroxy-4’-methoxyflavone and the methyl esters, semisynthetic derivatives of a mixture of ursolic and oleanolic acids, showed no activity against the tested microorganisms. These results suggest that the carboxyl group present in the triterpenes may contribute to antimicrobial activity.

scholarly journals Synthesis and Antimicrobial Activity of 4-Arylthio- and 4 Alkylthiofunctionalized Pyrazolo[1,5-a]pyrazines

2019 ◽  
Vol 85 (1) ◽  
pp. 58-66
Author(s):  
Yevhenii Hrynyshyn ◽  
Hanna Musiichuk ◽  
Olena Komarovska-Porokhnyavets ◽  
Oksana Is’kiv ◽  
Nataliia Moskalenko ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Structural Modification ◽  
Bromoacetic Acid ◽  
Phosphorus Pentasulfide ◽  
First Case ◽  
Test Culture ◽  
Exocyclic Methylene ◽  
Derivatives Of ◽  
Test Cultures

The reaction of pyrazolo[1,5-a]pyrazine-4(5H)ones with phosphorus tribromoxide in boiling benzene yielded 4-bromopyrazolo[1,5-a]pyrazines, and the thionation with phosphorus pentasulfide in pyridine at 90 °C led to pyrazolo[1,5-a]pyrazine-4(5H)thiones. The synthesized bromine derivatives are electrophilic, and thiones are nucleophilic substrates. Their subsequent structural modification in the first case was carried out by interaction with thiophenols, and in the second case was conducted with functional halogenoalkanes. It was shown that bromides react with substituted thiophenols in dimethylformamide in the presence of potassium carbonate at 90 °C to form 4-arylthiopyrazolo[1,5-a]pyrazines with yields of 65–83 %. 4-S-methyl-functionalized derivatives of pyrazole[1,5-a]pyrazines with yields of 60–78 % were easily obtained by the alkylation of pyrazole[1,5-a]pyrazin-4(5H)thiones with a-bromoketones, bromoacetic acid, ethyl bromoacetate and bromoacetonitrile in the K2CO3—DMF system at room temperature. The composition of all synthesized compounds is in agreement with the results of elemental analysis and mass spectra. Their structure is confirmed by NMR 1H and 13C spectra. In particular, in the NMR 1H spectra of 4-arylthiopyrazolo[1,5-a]pyrazines, in addition to the characteristic signals of the pyrazole and pyrazine nuclei, signals of protons of thioaryl substituents are present in the range of 7.04 –8.05 ppm, and in NMR spectra of the 1H 4-S-methylfunctionalized derivatives of pyrazole[1,5-a]pyrazines signals of exocyclic methylene protons are present at 4.11– 5.02 ppm. Promising derivatives with antibacterial activity against the test cultures S. aureus (MIC = 7.8 g/mL), M. luteum (MIC = 3.9 g/mL), and antifungal activity against the test culture of fungus A. niger (MIC = 7.8 g/mL) were determined among 4-S-substituted pyrazole[1,5-a]pyrazines as a result of studies of the antimicrobial activity.

scholarly journals Burkholderia thailandensis methylated hydroxy-alkylquinolines: biosynthesis and antimicrobial activity in co-cultures

2020 ◽  
Author(s):  
Jennifer R Klaus ◽  
Charlotte Majerczyk ◽  
Stephanie Moon ◽  
Natalie A. Epplera ◽  
Sierra Smith ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Secondary Metabolites ◽  
Soil Bacterium ◽  
Burkholderia Thailandensis ◽  
New Information ◽  
Therapeutic Development ◽  
Carbon Side Chain ◽  
Derivatives Of

ABSTRACTThe bacterium Burkholderia thailandensis produces an arsenal of secondary metabolites that have diverse structures and roles in the ecology of this soil-dwelling bacterium. In liquid co-culture experiments, B. thailandensis secretes an antimicrobial that nearly eliminates another soil bacterium, Bacillus subtilis. To identify the antimicrobial, we used a transposon mutagenesis approach. This screen identified antimicrobial-defective mutants with insertions in the hmqA, hmqC and hmqF genes involved in biosynthesis of a family of 2-alkyl-4(1H)-quinolones called 4-hydroxy-3-methyl-2-alkenylquinolines (HMAQs), which are closely related to the Pseudomonas aeruginosa 4-hydroxy-2-alkylquinolines (HAQs). Insertions also occurred in the previously uncharacterized gene BTH_II1576. Results confirm that BTH_II1576 is involved in generating N-oxide derivatives of HMAQs (HMAQ-NO) in B. thailandensis and that HMAQ-NOs are sufficient to eliminate B. subtilis in co-cultures. Moreover, synthetic HMAQ-NO is ∼50-fold more active than HMAQ. Both the methyl group and the length of the carbon side chain account for high activity of HMAQ-NO against B. subtilis. The results provide new information on the biosynthesis and activities of HMAQs and reveal new insight into how these molecules might be important for the ecology of B. thailandensis.IMPORTANCEThe soil bacterium Burkholderia thailandensis produces 2-alkyl-4(1H)-quinolones, mostly methylated 4-hydroxy-alkenylquinolines, a family of relatively unstudied metabolites similar to molecules also synthesized by Pseudomonas aeruginosa. Several of the methylated 4-hydroxy-alkenylquinolines have antimicrobial activity against other species. We show that N-oxidated methyl-alkenylquinolines are particularly antimicrobial and sufficient to kill Bacillus subtilis in co-cultures. We confirmed their biosynthesis requires the previously unstudied protein HmqL. These results provide new information about the biology of 2-alkyl-4(1H)-quinolones, particularly the methylated 4-hydroxy-alkenylquinolines, which are unique to B. thailandensis. This study also has importance for understanding B. thailandensis secondary metabolites and has implications for potential therapeutic development.

scholarly journals Synthesis, Characterization and Antimicrobial Activity of Some Novel 1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile Derivatives

2015 ◽  
Vol 11 (6) ◽  
pp. 3635-3641
Author(s):  
Monther Mahdi
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Research Work ◽  
Aromatic Aldehydes ◽  
Diffusion Method ◽  
Klebsiella Pneumonia ◽  
Pyrazole Derivative ◽  
Keto Ester ◽  
Derivatives Of

The present research work deals with synthesize a series of various substituted benzothiazole containing 6-amino- 4-(substituted aryl)- tetrahydropyrano[2,3-c]pyrazole-5-carbonitrilic by reacting 2-mercaptobenzothiazole with hydrazine hydrate to synthesize hydrazine derivatives of benzothiazole (1), which then reacted with β- keto ester to develop pyrazole derivative (2), and then finally reacted with malononitrile and different aromatic aldehydes to obtain the final compounds (3a-3f). The structures of the intermediates and final compounds are assigned by using FTIR and 1H-NMR. The final compounds were screened for their antibacterial activity against four tested bacteria as G+ and G- using a well diffusion method. The results of antibacterial activity exhibited that the species Klebsiella pneumonia was the most effected types, while Pseudomonas aeruginosa was least the effected in general. 

scholarly journals Synthesis of 1,2,3-triazole derivatives based on propargyl ester of a saturated single-basic carbonic acid and para-azidobenzoic acid

2021 ◽  
Vol 12 (1) ◽  
pp. 13-17
Author(s):  
Ibragimdjan Аbdugafurov Azizovich ◽  
Fazliddin Qirgizov Bakhtiyarovich ◽  
Ilhom Оrtikov Sobirovich
Keyword(s):  
Carbonic Acid ◽  
Effect Of Temperature ◽  
Reaction Yield ◽  
Factors Affecting ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
First Time ◽  
Derivatives Of ◽  
Membered Heterocycle

The development of highly effective and low-toxicity nonsteroidal anti-inflammatory drugs (NSAIDs) is one of the important challenges facing modern pharmacology. To overcome this problem, many studies have been conducted on compounds containing a five-membered heterocycle containing three nitrogen atoms. The pharmacodynamics of these compounds are mainly due to their anti-inflammatory effect. Therefore, it is important to synthesize new derivatives of 1,2,3-triazoles, to determine their structure and to look for substances with anti-inflammatory activity on their basis. For the first time, the corresponding derivatives of 4-(4-(exchangeable)-1H-1,2,3-triazole-1-yl)-benzoic acid were synthesized by cycloaddition of propargyl esters of saturated carboxylic acids and para-azidobenzoic acid in the presence of copper (I) iodide. The structure of the obtained substances was analyzed by IR, 1H NMR, and MS techniques. It is proved that under the action of the catalyst in the reaction, only 1,4-isomers are formed. Factors affecting the course of the reaction were identified. Only one isomer is formed in the reaction of cyclic addition under the action of a catalyst and the effect of temperature, duration of time, and nature of the solvent on the reaction yield was studied.

scholarly journals Determination of antimicrobial activity of some 1,2,4-triazole derivatives

2018 ◽  
Vol 9 (2) ◽  
pp. 203-208 ◽  
Author(s):  
M. S. M. Alrawashdeh
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Klebsiella Pneumonia ◽  
Pathological Changes ◽  
Infectious Bronchitis ◽  
E Coli ◽  
Compound Ii ◽  
Derivatives Of ◽  
Test Cultures

We carried out MIC of the derivatives of 1,2,4-triazole II (4-((5-nitrofuran-2-yl)methyleneamino)-1-propyl-4H-1,2,4-triazolium bromide) and I (N-((5-nitrofuran-2-yl)methylene)-4H-4-amino-1,2,4-triazolidium chloride) against Escherichia coli ATCC 3912/4 and E. coli k88ad, Staphylococcus aureus ATCC 25923 and S. aureus k99, Klebsiella pneumonia k56 and Salmonella typhimurium 144, S. enteritidis. All test cultures were sensitive to compound II at concentrations of 1,25–0,039 μg/ml. Similar MIC (0,039 μg/ml) of compounds II and I were set for E. coli k88a and S. aureus k99 test cultures – 0,156 μg/ml. Only S. aureus ATCC 25923 and K. pneumonia k56 had sensitivity to ceftriaxone (MIC = 0,097 μg/ml). Antiviral activity of Trifuzol (piperidine 2-[5-(furan-2-il)-4-phenil-1,2,4-triazol-3-ilthio]acetate) and avistim (morpholines 3-(4-pyridyl)-1,2,4-triazolil-5-thioacetate) against the chicken infectious bronchitis virus (VIB) strain 4/91 was characterized by a decrease in mortality and pathological changes of chicken embryos (CE) which were induced by the virus. Death of infected CE provoked by the strain 4/91 of VIB in dilution 10–3 occurred at 57.1%. The reduction in the percentage of deaths of CE infected by the virus in dilution 10–3 in the presence of Avistim was 28.6%, and with Trifuzol 14.3%. The use of avistim and Trifuzol compounds reduced VIB infectious activity when it was cultivated in CE, reducing the titre of the virus (strain 4/91) by 3 lg EID 50 cm–3.

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 C-3 Substituted Lawsonemonoximates of Holmium(III): Synthesis, Characterization, and Antimicrobial Activity

2000 ◽  
Vol 7 (3) ◽  
pp. 147-150 ◽  
Author(s):  
S. B. Jagtap ◽  
S. G. Joshi ◽  
G. M. Litake ◽  
V. S. Ghole ◽  
B. A. Kulkarni
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antimicrobial Effect ◽  
Diffusion Method ◽  
Disk Diffusion Method ◽  
E Coli ◽  
Mueller Hinton ◽  
Providencia Stuartii ◽  
Derivatives Of ◽  
Klebsiella Spp

A series of five new metal complexes of Ho(III) with C-3 substituted derivatives of lawsonemonexime (2-hydroxy-1,4-naphthalenediene-1-oxime) were synthesized. The compounds were characterized by melting point, elemental analysis, IR spectroscopy and magnetic susceptibility. The antimicrobial activity of the compounds were determined by disk diffusion method and broth micro-dilution techniques using Mueller Hinton medium against the following organisms: S. aureus ATCC 6538P, Klebsiella pneumoniae, NCTC 418, Pseudomonas aeruginosa ATCC 27833, Salmonella typhimurium ATCC 23564, E. coli U 1777, E. coli HB101, Proteus morganii NCIM 2860, Providencia stuartii NCIM 2799 and Acinetobacter baumannii U 24. The chelates of Ho(III) with lawsonemonoxime and Ho(III) with 3-bromolawsonemonoxime showed a variable antimicrobial activity against all organisms tested except Pseudomonas and Klebsiella spp. S. aureus was found more sensitive to all ligands and chelates tested; but the MIC values of chelates were considerably less; thus having more antimicrobial effect.

scholarly journals Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol

2021 ◽  
pp. 64-69
Author(s):  
Yevhen Karpun ◽  
Nataliia Polishchuk
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Biological Screening ◽  
Antimicrobial Substances ◽  
Pharmaceutical Ingredients ◽  
Wide Range ◽  
Derivatives Of

The aim of the work. 1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol series, and study some regularities of the “structure – biological activity” relationship for the synthesized compounds as well. Materials and methods. The subject of the study was new S-substituted 1,2,4-triazoles containing 2-oxopropan-1-yl and 2-aryl-2-oxoethan-1-yl substituents. The antimicrobial activity was studied by double serial dilutions on test cultures of Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 885-653). The results of the biological screening showed that at a concentration of 125 g/mL, all synthesized substances showed activity (MIC – in the range of 31.25 - 62.5 μg/mL, MBCK - in the range of 62.5–125 μg/mL) against strains of Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans. Variation of substituents on the sulfur atom did not lead to a significant change in antimicrobial and antifungal activities among derivatives of 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl) thio)methyl)-4H-1,2,4-triazole-3-thiols. Conclusions. Biological screening data indicate the prospects for the search for new antimicrobial substances among the abovementioned derivatives of 1,2,4-triazoles. The most active compounds were 1-((4-ethyl-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)propan-2-one and 1-(4-methoxyphenyl)-2-(4-ethyl-5-(((3-(pyridin-4-yl)-1H)-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazol-3-yl)thio)ethanone, which showed the most pronounced antimicrobial activity against the Pseudomonas aeruginosa strain (MIC – 31.25 μg/mL, MBcK - 62.5 μg/mL)

The Study of Bacillus Subtils Antimicrobial Activity on Some of the Pathological Isolates

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Hussein A Kadhum ◽  
Thualfakar H Hasan2
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Bacterial Growth ◽  
Broad Spectrum ◽  
Inhibitory Activity ◽  
Bacterial Pathogens ◽  
Inhibitory Ability ◽  
Selection Of

The study involved the selection of two isolates from Bacillus subtilis to investigate their inhibitory activity against some bacterial pathogens. B sub-bacteria were found to have a broad spectrum against test bacteria such as Staphylococcus aureus and Pseudomonas aeruginosa. They were about 23-30 mm and less against Klebsiella sp. The sensitivity of some antibodies was tested on the test samples. The results showed that the inhibitory ability of bacterial growth in the test samples using B. subtilis extract was more effective than the antibiotics used.

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