scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

scholarly journals Synthesis and Evaluation of Some Novel Chromone Based Dithiazoles as Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Naureen Aggarwal ◽  
Vishal Sharma ◽  
Harpreet Kaur ◽  
Mohan Paul Singh Ishar
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Fungal Strains ◽  
Inhibitory Potential ◽  
C Nmr

Novel substituted 1,2,4-dithiazolylchromones 3a–j were synthesized by the reaction of 3-formylchromones (1a–j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.

scholarly journals Synthesis and Antimicrobial Activity of Coumarinyl Schiff Base Derivatives

2014 ◽  
Vol 30 ◽  
pp. 193-201 ◽  
Author(s):  
Arun Mishra ◽  
Jaynt Rathod ◽  
Dipti Namera ◽  
Shailesh Thakrar ◽  
Anamik Shah
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Gram Negative ◽  
H Nmr ◽  
Schiff Base Derivatives ◽  
Test Organisms ◽  
Ft Ir ◽  
C Nmr

We have reported some novel N’-[(1)-ethylidene]-2-(6-methyl-2-oxo-2H-chromen-4-yl) acetohydrazide synthesized by conventional method. The reaction of 2-(6-methyl-2-oxo-2H-chromen-4-yl)acetohydrazide with substituted benzaldehyde in methanol as a solvent yielded a series of (7a-l). The structures of all synthesized compounds are well characterized by Mass, FT-IR, 1H NMR, 13C NMR and elemental analysis. Moreover, all synthesized compounds were screened for In Vitro antimicrobial activity against the gram positive (Staphylococcus aureus, Bacilluas subtilis) and gram negative (Escherichia coli, P. aeruginosa, K. pneunonae, Enterobacter) bacterial strain. In which some the compounds show potential inhibition against the test organisms.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

Synthesis, in vitro inhibition effect of novel phthalocyanine complexes as carbonic anhydrase and paraoxonase enzyme inhibitors

2020 ◽  
Vol 24 (08) ◽  
pp. 1047-1053
Author(s):  
Emre Güzel ◽  
Barış Seçkin Arslan ◽  
Kübra Çıkrıkçı ◽  
Adem Ergün ◽  
Nahit Gençer ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Enzyme Inhibitors ◽  
Inhibition Effect ◽  
H Nmr ◽  
Vis Spectroscopy ◽  
Ft Ir ◽  
First Time ◽  
Ft Ir Spectroscopy ◽  
C Nmr

The preparation and assessment of carbonic anhydrase and paraoxonase enzyme inhibition properties of 3-(2-(5-amino-4-(4-bromophenyl)-3-methyl-1H-pyrazol-1-yl)ethoxy)phthalonitrile (2) and its nitrogen-containing non-peripheral phthalocyanine derivatives (3 and 4) are reported for the first time. The new phthalonitrile and its phthalocyanine derivatives have been elucidated by FT-IR spectroscopy, 1H-NMR, [Formula: see text]C-NMR, mass and UV-vis spectroscopy. The results demonstrated that all synthesized compounds moderately inhibited carbonic anhydrase and paraoxonase enzymes. Among the compounds, the most active ones were found to be compound 4 for PON (Ki : 0.14 [Formula: see text]M), compound 3 for hCA I (Ki : 22.52 [Formula: see text]M) and compound 1 for hCA II (Ki : 13.62 [Formula: see text]M).

scholarly journals Synthesis and Antimicrobial Activity ofSome New 2-Substituted Benzothiazole Derivatives

2009 ◽  
Vol 6 (3) ◽  
pp. 775-779 ◽  
Author(s):  
B. Rajeeva ◽  
N. Srinivasulu ◽  
S. M. Shantakumar
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
Diffusion Method ◽  
Disc Diffusion ◽  
Phosphoryl Chloride ◽  
Mass Spectral Data ◽  
Disc Diffusion Method ◽  
Mass Spectral ◽  
Benzothiazole Derivatives ◽  
H Nmr

Some new 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3- benzothiazole(3a-j)were synthesized by refluxing benzothiazolyl carboxyhydrazide with different aryl acids in phosphoryl chloride. Structures of the synthesized compounds were established on the basis of1H NMR and Mass spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.

scholarly journals Approach for the Synthesis of Potent Antimicrobials Containing Pyrazole, Pyrimidine and Morpholine Analogues

2016 ◽  
Vol 69 ◽  
pp. 87-96 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Bonny Y. Patel ◽  
Bharti P. Dave
Keyword(s):  
Antimicrobial Activity ◽  
Dilution Method ◽  
Mass Spectral ◽  
H Nmr ◽  
Sar Studies ◽  
Mueller Hinton ◽  
Morpholine Derivatives ◽  
Mueller Hinton Broth ◽  
C Nmr

The present study is in the interest of some synthesized novel derivatives containing 4-(1,3-diphenyl-1H-pyrazol-4-yl)-N-(morpholinomethyl)-6-arylpyrimidin-2-amines pooled with different bio-active heterocycles such as pyrazole, pyrimidine and morpholine derivatives. The structures of newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial activity against different bacterial and fungal strains using Mueller-Hinton Broth dilution method. On the basis of SAR studies, it was observed that the presence of electron withdrawing groups remarkably enhanced the antimicrobial activity of synthesized compounds.

scholarly journals A Novel Cd(II) Isophthalate Complex with Triethanolamine: Crystal Structure, Fluorescence and Antimicrobial Activity

2021 ◽  
Vol 68 (2) ◽  
pp. 466-474
Author(s):  
Zuhal Yolcu ◽  
Sinem Yurtcan ◽  
Meryem Çıtlakoğlu
Keyword(s):  
Antimicrobial Activity ◽  
Room Temperature ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Single Crystal Diffraction ◽  
X Ray ◽  
Ft Ir ◽  
First Time ◽  
Trigonal Prismatic

A mixed ligand Cd(II) complex [Cd(IsoPht)(TEA)H2O]·3H2O was synthesized for the first time by using isophthalic acid (H2IsoPht) and tetradentate triethanolamine (TEA) and characterized by X-ray single-crystal diffraction, FT-IR, and thermogravimetric analysis (TGA). This novel complex crystallizes in the triclinic system with P-1 space group and distorted monocapped trigonal prismatic geometry. The Cd(II) has seven coordinates with bidentate IsoPht, a TEA in the tetradentate mode, and an aqua ligand. The fluorescence properties of the Cd(II) complex and TEA ligand were investigated at room temperature. The present Cd(II) complex was also tested for its antimicrobial activity by in vitro agar diffusion method against some Gram-positive and Gram-negative bacteria and a fungus.

scholarly journals Synthesis of Thiophenyl Thiazole Based Novel Quinoxaline Derivatives

2015 ◽  
Vol 51 ◽  
pp. 115-124
Author(s):  
Haresh G. Kathrotiya ◽  
Yogesh T. Naliapara
Keyword(s):  
Aromatic Amine ◽  
Elemental Analysis ◽  
Condensation Reaction ◽  
High Yield ◽  
Experimental Procedure ◽  
H Nmr ◽  
Quinoxaline Derivatives ◽  
Ft Ir ◽  
C Nmr

A new series of thiophenyl thiazole based novel quinoxaline derivatives 4a-4t have been synthesized by base catalysed condensation reaction. In which 6-substituted 2,3-dichloroquinoxaline 1a and 4-(thiophen-2-yl) thiazol-2-amine 2b reacted in basic condition to afford intermediate 3c which reacts with various aromatic amine to form final compounds. Easy experimental procedure, high yield, and selectivity are the imperative features of this method. The identity of all the compounds has been established by 1H NMR, 13C NMR, FT-IR, and elemental analysis.

scholarly journals Isolation and Antimicrobial Activity of β-Sitosterol-3-O-Glucoside from Lannea Kerstingii Engl. & K. Krause (Anacardiacea)

2016 ◽  
Vol 06 (01) ◽  
pp. 004-008
Author(s):  
Njinga N. S. ◽  
Sule M. I. ◽  
Pateh U. U. ◽  
Hassan H. S. ◽  
Abdullahi S. T. ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Wide Spectrum ◽  
Diffusion Method ◽  
Dilution Method ◽  
Minimum Fungicidal Concentration ◽  
E Coli ◽  
H Nmr ◽  
Vacuum Liquid Chromatography ◽  
Broth Dilution ◽  
C Nmr

AbstractThe emergence of more and more drug resistance bacteria has led to the study of the antimicrobial activity of the compound isolated from Lannea kerstingii Engl. & K. Krause (Anacardiacea) since the active principles of many drugs found in plants are secondary metabolites. A compound was isolated using dry vacuum liquid chromatography and eluting with CHCl3 -EtOAc and monitored using TLC. 3 1 13 The glycoside was characterized using 1 H NMR and 13 C NMR spectra recorded in DMSO-d6 at 400 MHz and 125 MHz, respectively. The antimicrobial activity of the compound was determined using agar diffusion method. The minimum inhibitory concentration (MIC) and minimum bactericidal/minimum fungicidal concentration (MBC/MFC) was determined using broth dilution method. The compound isolated was found to be β-sitosterol-3-O-glucoside. The β-sitosterol-3-O-glucoside (200μg/ml) was active against S. aureus, Methicillin Resistant Staphylococcus aureus, P. mirabilis, S. typhi, K. pneumoniae, E. coli, B. subtilis with zone of inhibition ranging from 24mm to 34mm and inactive against P. aeroginosa and Proteus vulgaris. It was also active against the fungi C. albicans and C. tropicalis but inactive against C. krusei. The MIC ranged from 25 to 50 μg/ml while the MBC/MFC ranged from 50 to 200 μg/ml. These results show the wide spectrum antimicrobial activity of β-sitosterol-3-O-glucoside.

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