scholarly journals Synthesis and Evaluation of Antimicrobial Activities of New Functional Derivatives of 3-[5-(4-Nitrophenyl)-2-Furyl]-4-Pyrazole-Carbaldehydes

2021 ◽  
Vol 11 (4) ◽  
pp. 12159-12169
Keyword(s):  
1H Nmr ◽  
Antimicrobial Agents ◽  
Ethyl Cyanoacetate ◽  
Synthesis Method ◽  
Antimicrobial Activities ◽  
E Coli ◽  
Functional Derivatives ◽  
Composition And Structure ◽  
Biological Potential ◽  
Derivatives Of

The analysis of the biological potential of derivatives of 4-alkenyl- and imino functionalized pyrazoles is carried out, based on which the expediency of design of new structures with pharmacophore 5-(4-nitrophenyl)furanyl fragment is substantiated. Their synthesis method using a structural modification of 3-[5-(4-nitrophenyl)furan-2-yl]pyrazole-4-carbaldehyde to the corresponding alkenyl derivatives under the action of malononitrile, ethyl cyanoacetate, cyanoacetamide, and thioxoimidazolidine is proposed. The hydrazones, (thio)semicarbazones, and oximes were obtained by the condensation of corresponding aldehydes with hydrazides, (thio)semicarbazides, and hydroxylamine. The synthesized compounds' composition and structure were determined by elemental analysis, IR, and 1H NMR spectra. The fact existence of a mixture of E/Z-isomers among the series of obtained hydrazones of 1-phenyl-4-pyrazolecarbaldehydes was determined, and the quantitative ratio of geometric isomers was determined using 1H NMR spectroscopy data. The results of the microbiological evaluation of the synthesized pyrazole derivatives showed that they have a pronounced effect on strains of bacteria S. aureus ATCC 25923, E. coli ATCC 25922, and fungi of the genus Candida and are promising for the creation of effective antimicrobial agents.

scholarly journals Microbial Transformations of Isophorone by Alternaria alternata and Neurospora crassa

2013 ◽  
Vol 8 (1) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Ismail Kiran ◽  
Özge Özşen ◽  
Turgay Çelik ◽  
Semra İlhan ◽  
Bükay Yenice Gürsu ◽  
...  
Keyword(s):  
Neurospora Crassa ◽  
Alternaria Alternata ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Anti Oxidant ◽  
Agar Dilution ◽  
Important Field ◽  
Pharmacology And Toxicology ◽  
Derivatives Of

Isophorone (3,5,5-trimethyl-2-cyclohexen-1-one), a monoterpene, and the structurally related 1,8-cineole and camphor, have demonstrated a protective effect against cancer, biological activity against a variety of microorganisms, and anti-oxidant properties. The derivatization of isophorone is, therefore, an important field of xenobiochemistry, pharmacology and toxicology. The aim of this study was to obtain derivatives of isophorone through microbial biotransformation and evaluate the biotransformation metabolites as potential antimicrobial agents. Incubation of isophorone with the fungi Alternaria alternata and Neurospora crassa afforded 4α-hydroxy- and 7-hydroxy-isophorone as transformation metabolites. The antimicrobial activities of isophorone and the metabolites were evaluated in vitro both by using agar dilution and microdilution methods. However, no significant antibacterial activity was observed when compared with those of standard substances.

scholarly journals DPPH-Scavenging and Antimicrobial Activities of Asteraceae Medicinal Plants on Uropathogenic Bacteria

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Phan-Canh Trinh ◽  
Le-Thi-Thanh Thao ◽  
Hoang-Tran-Viet Ha ◽  
TuAnh Nguyen
Keyword(s):  
Antimicrobial Agents ◽  
Natural Antioxidants ◽  
Ethyl Acetate Fraction ◽  
Antimicrobial Activities ◽  
Chrysanthemum Morifolium ◽  
Bacterial Strains ◽  
Ageratum Conyzoides ◽  
Potent Effect ◽  
E Coli ◽  
Dpph Scavenging

Asteraceae species were widely applied in traditional medicines in Asian countries as sources of natural antioxidants and antimicrobial agents. This study aimed to evaluate DPPH-scavenging capacities and antimicrobial activities of nine Asteraceae species collected from Southern Vietnam. Antioxidant and antimicrobial activities were determined by standard protocols. Essential oils from Ageratum conyzoides, Helianthus annuus, and Artemisia vulgaris indicated significant inhibitory effects on Staphylococcus aureus and Candida spp. Crude extracts and fractions from Taraxacum officinale, Chrysanthemum morifolium, A. conyzoides, and Tagetes erecta showed inhibitory ability on at least one testing bacterial strains including S. aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. In a study on clinical isolates, ethyl acetate fraction from A. conyzoides flower displayed the most potent effect on uropathogenic E. coli and K. pneumoniae with MIC at 1.25–10 mg/ml and 5–12.5 mg/ml, respectively. DPPH-scavenging assay indicated that T. erecta extract had the lowest IC50 (17.280 μg/ml) and is 2.4 times higher than vitamin C (7.321 μg/ml). This study revealed that A. conyzoides has good potential against uropathogenic E. coli and K. pneumoniae, and therefore could be applied for prophylactic treatment of urinary infection.

scholarly journals Synthesis, Characterization, and Thermal and Antimicrobial Activities of Some Novel Organotin(IV): Purine Base Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik
Keyword(s):  
Antimicrobial Agents ◽  
Rhizopus Oryzae ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Purine Base ◽  
Mass Spectral ◽  
E Coli ◽  
Kinetic And Thermodynamic Parameters ◽  
C Nmr

A new series of organotin(IV) complexes with purine bases theophylline (HL1) and theobromine (L2) of the types R3Sn(L1), R2Sn(L1)Cl, R3Sn(L2)Cl, and R2Sn(L2)Cl2(R = C6H5CH2–;p-ClC6H4CH2–) have been synthesized in anhydrous THF. The complexes were characterized by elemental analysis, conductance measurements, molecular weight determinations, UV-vis, IR,1H,13C NMR, and mass spectral studies. Various kinetic and thermodynamic parameters of these complexes have also been determined using TG/DTA technique. The thermal decomposition techniques indicate the formation of SnO2as a residue. The results show that the ligands act as bidentate, forming a five-member chelate ring. All the complexes are 1 : 1 metal-ligand complexes. In order to assess their antimicrobial activity, the ligands and their corresponding complexes have also been testedin vitroagainst bacteria (E. coli, S. aureus, andP. pyocyanea) and fungi (Rhizopus oryzaeandAspergillus flavus). All the complexes exhibit remarkable activity, and the results provide evidence that the studied complexes might indeed be a potential source of antimicrobial agents.

scholarly journals SYNTHESIS CHARACTERIZATION AND ANTIMICROBIAL ACTIVITIES STUDIES OF N-{2-(4-CHLOROPHENYL) ACETYL} AMINO ALCOHOLS DERIVED FROM α-AMINO ACIDS

2020 ◽  
pp. 11-16
Author(s):  
G. Venkateshappa ◽  
G. Shivaraju ◽  
P. Raghavendra Kumar
Keyword(s):  
Amino Acids ◽  
Amino Alcohols ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Moderate Activity ◽  
E Coli ◽  
Synthetic Drugs ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Derivatives Of

Amino acids play important roles in organisms to sustain in living state and perform as body constituents, enzymes and antibodies. At insalubrious situations, use of amino acids derivatives as drugs in the maintenance of normal health is better choice than common unnatural synthetic drugs. This is due to the fact that the amino acids derivatives may be more bio-compatible, biodegradable and eliminate easily than others.  In this sense we have made an effort and report herein the synthesis of N-{2-(4-chlorophenyl) acetyl} amino alcohols synthesised by reduction of N-{2-(4-chlorophenyl)acetyl} derivatives of (S)-amino acids such as (S)-phenylalanine, (S)-alanine, (S)-methionine, (S)-leucine, (S)-tryptophan and (S)-proline. These newly synthesized amino acids derivatives were analysed by proton, carbon-13 NMR and FT-IR spectroscopy. The composition of solid derivatives was determined by elemental analysis. Further, antimicrobial activities of these derivatives were assessed on usual bacteria K. aerogenes, E. coli, S. aureus and P. desmolyticum and fungi A. flavus and C. albicans. The compounds were witnessed moderate activity than authorised antibacterial and fungal agents Ciprofloxacin and Fluconazole respectively. The antimicrobial studies also revealed that, these derivatives could be better antifungal agents than antibacterial agents. Finally we compared the experimental results of antimicrobial activities with docking studies.  

scholarly journals Synthesis of sulfonamides bearing 1,3,5-triarylpyrazoline and 4-thiazolidinone moieties as novel antimicrobial agents

2020 ◽  
Vol 85 (2) ◽  
pp. 155-162
Author(s):  
Thi-Dan Thach ◽  
Thi Le ◽  
Thien-Annguyen Nguyen ◽  
Chi-Hien Dang ◽  
Van-Su Dang ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Significant Inhibition ◽  
Mercaptoacetic Acid ◽  
Bacterial Strains ◽  
Reference Drug ◽  
E Coli ◽  
Yeast Strains ◽  
Microbial Strains

Two series of sulfonamides were synthesized from 4-hydrazinylbenzenesulfonamide as the key starting material. 1,3,5-Triarylpyrazoline sulfonamides (2a?i) were obtained by cyclocondensation of various chalcones in 53? ?64 % yields, while 4-thiazolidinone derivatives (4a?e) were synthesized by cyclocondensation between mercaptoacetic acid and different phenylhydrazones in 43?62 % yields. The synthesized compounds were characterized based on FTIR, 1H-NMR, 13C-NMR and HRMS data. The sulfonamides were evaluated for their in vitro antimicrobial activities against four bacterial strains (E. coli, P. aeruginosa, B. subtillis and S aureus), two filamentous fungal strains (A. niger and F. oxysporum) and two yeast strains (C. albicans and S. cerevisiae). Seven pyrazolines, 2a?c and 2e?h, exhibited significant inhibition of different microbial strains. Among them, compound 2b displayed good antifungal activity against A. niger (MIC value at 12.5 ?g mL-1) over the reference drug.

scholarly journals Synthesis and Antimicrobial Evaluations of Sulfur Inserted Fluoro-Benzimidazoles

2021 ◽  
Vol 33 (7) ◽  
pp. 1525-1529
Author(s):  
Parmesh Kumar Dwivedi ◽  
Devdutt Chaturvedi
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Strains ◽  
Substituted Anilines ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
New Compounds ◽  
Derivatives Of ◽  
Multiple Step

A new series of fluorinated sulfur inserted benzimidazole analogues Za-i were synthesized and characterized. The new compounds were screened for their antimicrobial and antioxidant potential. The synthesized compounds were obtained by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol X. The compounds Ya-i prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF. Finally, the compound X was reacted with different derivatives of 2-chloro-N-phenylacetamide resulting in formation of titled compounds Za-i. The synthesized compounds (Za-Zi) were characterized by spectral analysis viz.1H & 13C NMR, mass spectra, elemental analysis and IR. The in vitro antimicrobial potential against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans) was recorded for the obtained compounds. Some of the compounds exhibited encouraging results (in MIC) against Gram-positive and Gram-negative bacterial strains. These studies thus suggest that the designed sulfur inserted fluoro-benzimidazoles scaffold may serve as new promising template for further amplification as antimicrobial agents.

scholarly journals Efficiency of Basil Essential Oil Antimicrobial Agents under Different Shading Treatments and Harvest Times

Agronomy ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 1574
Author(s):  
Zoran S. Ilić ◽  
Lidija Milenković ◽  
Ljubomir Šunić ◽  
Nadica Tmušić ◽  
Jasna Mastilović ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Plant Production ◽  
Exposure Control ◽  
Harvest Time ◽  
E Coli ◽  
Growing Conditions

The aim of this study was to determine the antimicrobial activity of essential oils obtained from sweet basil (Ocimum basilicum L. cv. ‘Genovese’) cultivated in the open field under different shading conditions (red, blue, and pearl nets with a shade index of 50% and full sunlight exposure (control plants)), harvested at different times. The antimicrobial activity of basil essential oils (BEOs) obtained from all samples was determined for four microorganisms, while determinations for an additional five microorganisms included samples from non-shaded plants, plants grown under red and pearl nets, and second harvest of plants grown under blue net. Basil essential oil exhibited antimicrobial activity surpassing the activity of relevant commercial antibiotics regardless of growing conditions in the case of B. cereus, K. pneumoniae and C. albicans, while superior antimicrobial activity was exhibited in the case of essential oils from plants grown under blue nets in the case of S. aureus, E. coli and P. vulgaris. The influence of the application of colored shading nets was highly significant (p < 0.01) in the cases of all analyzed microorganisms except C. albicans and P. aeruginosa, while the influence of harvest time was proven in the cases of all microorganisms except K. pneumoniae. ANOVA proved that antimicrobial activities are highly dependent on the methods of plant production, shading treatment, and harvest time. Obtained results are discussed in relation to previously determined composition and yield of essential oils from basil grown under shade nets and harvested in different periods.

scholarly journals Antimicrobial Activities of Cymbopogon citratus and Ximenia Americana Leaf Extracts Against Some Selected Bacterial and Yeast Clinical Isolates

2021 ◽  
pp. 1-10
Author(s):  
A. U. Hassan ◽  
A. H. Madu ◽  
U. O. Ozojiofor ◽  
A. H. Galadanci ◽  
I. B. Mato ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Cymbopogon Citratus ◽  
Leaf Extracts ◽  
Phytochemical Content ◽  
E Coli ◽  
Plant Parts ◽  
Ximenia Americana ◽  
Bioassay Technique ◽  
Emergence Of Resistance

Increasing emergence of resistance to antibiotics by pathogenic microorganisms worldwide necessitates the need for finding new antimicrobial agents with minimal resistance and side effects. This study was carried out to investigate the phytochemical content and antimicrobial activities of two ethno-medicinal plants namely: Cymbopogon citratus and Ximenia Americana. Methanol and aqueous were used as solvent for a soxhlet and aqueous percolation extraction techniques to obtain the crude extracts of the named plant parts. Tannins, steroids, reducing sugars, tritapenoids and Flavonoids were found present in these plant extracts. GC-MS analysis done in this study indicates the presence of some basic phenolic compounds, such as; Cyclohexane-1-3,5-trione & 2-phenyl-1,4-benzopyrone, in the C. citratus extract and methyl guanidine & 3-meyhylheptyl acetate in the X. americana extract, which have been attributed with numerous antimicrobial effects onmicrobial pathogens. Using an agar well diffusion bioassay technique the C. citratus extracts shows; both the extracts are active against E. coli and P. aeroginosa. While X. americana extracts shows a higher activity against C. albican. However the MIC/MBC/MFC of all the extracts shows that known of the extracts has an active viability below 12.5µg/ml.

scholarly journals Cytotoxic Activity-Guided Isolation from Achillea monocephala, and Biological Activities of its Different Extracts

2020 ◽  
Vol 8 (1) ◽  
pp. 7-14
Author(s):  
Turgut Taşkın ◽  
Eray M. Güler ◽  
Şeyda Şentürk ◽  
Damla D. Çelik ◽  
Turan Arabacı ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cytotoxic Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Cytotoxic Activities ◽  
Active Compounds ◽  
Antioxidant Power ◽  
Biological Potential

Background: The genus Achillea is one of the most important genus of the Asteraceae family and many species of Achillea are used in traditional medicine to treat several ailments. Aim: The aim of the current research was to evaluate in vitro cytotoxic activities of n-hexan, chloroform, ethyl acetate and methanol extracts and to isolate the active compounds from the extract showing the strongest cytotoxic activity. In addition to this, it was aimed to evaluate the biological activities (cytotoxic, antioxidant, anti-urease, anticholinesterase, antimicrobial) of different extracts and active compounds from Achillea monocephala. Methods and Materials: The in vitro antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial activities of different extracts from A. monocephala aerial parts were examined. The structures of the active compounds were determined by NMR techniques, UV, IR and LC-MS/MS analysis and their biological potential was examined. Results: The chloroform extract showed strong and selective cytotoxic activity on the cancer cell lines (MDA-MB-231, MCF-7). Besides, this extract exhibited stronger antimicrobial activity than other extracts. Therefore, through activity-guided procedures, luteolin, naringenin and 8-hydroxy-salvigenin compounds were isolated from this extract. The methanol extract showed stronger antioxidant (DPPH, ABTS, CUPRAC) and anticholinesterase activity than other extracts. The n-hexan extract exhibited the highest anti-urease activity. In this study, it was determined that the isolated compounds had a strong biological activity. Naringenin compound had stronger ABTS radical cation scavenging and ferric reducing/antioxidant power, cytotoxic and antimicrobial activity than other compounds. 8-hydroxy-salvigenin compound showed the highest urease and acetylcholinestease enzyme inhibition. Conclusion: The results of this study suggest that the extracts and isolated compounds from the A. monocephala may be used as antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial agents in the future.

scholarly journals Synthesis and Biological Evaluation of 1,2,3-Triazole Tethered Thymol-1,3,4-Oxadiazole Derivatives as Anticancer and Antimicrobial Agents

2021 ◽  
Vol 14 (9) ◽  
pp. 866
Author(s):  
Abdulraheem S. A. Almalki ◽  
Syed Nazreen ◽  
Azizah M. Malebari ◽  
Nada M. Ali ◽  
Ahmed A. Elhenawy ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Standard Drug ◽  
E Coli ◽  
Hct 116 ◽  
Oxadiazole Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Better Than ◽  
Mcf 7

A library of 1,2,3-triazole-incorporated thymol-1,3,4-oxadiazole derivatives (6–18) hasbeen synthesized and tested for anticancer and antimicrobial activities. Compounds 7, 8, 9, 10, and 11 exhibited significant antiproliferative activity. Among these active derivatives, compound 2-(4-((5-((2-isopropyl-5-methylphenoxy)methyl)-1,3,4-oxadiazol-2-ylthio)methyl)-1H-1,2,3-triazol-1-yl)phenol (9) was the best compound against all three tested cell lines, MCF-7 (IC50 1.1 μM), HCT-116 (IC50 2.6 μM), and HepG2 (IC50 1.4 μM). Compound 9 was found to be better than the standard drugs, doxorubicin and 5-fluorouracil. These compounds showed anticancer activity through thymidylate synthase inhibition as they displayed significant TS inhibitory activity with IC50 in the range 1.95–4.24 μM, whereas the standard drug, Pemetrexed, showed IC50 7.26 μM. The antimicrobial results showed that some of the compounds (6, 7, 9, 16, and 17) exhibited good inhibition on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). The molecular docking and simulation studies supported the anticancer and antimicrobial data. It can be concluded that the synthesized 1,2,3-triazole tethered thymol-1,3,4-oxadiazole conjugates have both antiproliferative and antimicrobial potential.

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