scholarly journals Synthesis and Antimicrobial Assessment of Some New 2-(Thiazol-5-yl)-1,3,4-oxadiazoles

2019 ◽  
Vol 70 (6) ◽  
pp. 1996-1999
Author(s):  
Catalin Araniciu ◽  
Smaranda Dafina Oniga ◽  
Cristina Ioana Stoica ◽  
Mariana Carmen Chifiriuc ◽  
Marcela Popa ◽  
...  

Considering the promising antimicrobial activity of compounds bearing the thiazole or the oxadiazole rings in their structures, we set out to obtain new antimicrobial molecules bearing the 2-(thiazol-5-yl)-1,3,4-oxadiazole schaffold. The structures of the 8 new compounds obtained was confirmed by physicochemical characterization including: 1H-NMR, MS and elemental analysis. Antimicrobial activity was investigated against 5 Gram-positive bacterial strains, 2 Gram-negative bacterial strains and 2 fungal strains. The newly synthesized compounds showed modest antimicrobial activity.

2011 ◽  
Vol 65 (1) ◽  
Author(s):  
Carmen Limban ◽  
Alexandru Missir ◽  
Ileana Chirita ◽  
George Nitulescu ◽  
Miron Caproiu ◽  
...  

AbstractNew acylthiourea derivatives, 2-((4-ethylphenoxy)methyl)-N-(phenylcarbamothioyl)benzamides, were tested by qualitative and quantitative methods on various bacterial and fungal strains and proved to be active at low concentrations against Gram-positive and Gram-negative bacteria as well as fungi. These compounds were prepared by the reaction of 2-((4-ethylphenoxy)methyl)benzoyl isothiocyanate with various primary aromatic amines, and were characterised by melting point and solubility. The structures were identified by elemental analysis, 1H and 13C NMR, and IR spectral data. The level of antimicrobial activity of the new 2-((4-ethylphenoxy)methyl)benzoylthiourea derivatives was dependent on the type, number and position of the substituent on the phenyl group attached to thiourea nitrogen. The iodine and nitro substituents favoured the antimicrobial activity against the Gram-negative bacterial strains, while the highest inhibitory effect against Gram-positive and fungal strains was exhibited by compounds with electron-donating substituents such as the methyl and ethyl groups.


Author(s):  
Ankita A. Bhalu ◽  
Pooja Moteriya ◽  
Sumitra Chanda ◽  
Shipra H. Baluja

Some new dihydropyrano[c]chromenes derivatives are synthesized from 4-hydroxycoumarin. The structure of newly synthesized compounds was confirmed by mass, 1H NMR and IR spectroscopy. Further, antimicrobial screening of these synthesized compounds was done against some bacterial (Gram positive as well as Gram negative) and fungal strains in N,N-dimethylformamide. It is observed that some of synthesized compounds exhibited significant antibacterial activity against Gram positive bacterial strains. The selected fungal strains were most resistant for the studied compounds as none of the synthesized compounds showed activity against any of the fungal strain studied. The best antibacterial activity was shown by ABR-10.


2015 ◽  
Vol 10 (4) ◽  
pp. 765 ◽  
Author(s):  
Alia Erum ◽  
Sajid Bashir ◽  
Shazia Saghir

<p class="Abstract">Arabinoxylan is a polysaccharide of<em> Plantago ovata</em>, an indigenous plant of Pakistan and several European countries. In the present investigation arabinoxylan isolated from <em>P. ovata</em> husk was chemically modified i.e., carboxymethylated and was converted into its sodium salt. Physicochemical characterization of modified arabinoxylans was done. The antimicrobial assay of arabinoxylan and modified arabinoxylans was done by Kirby-Bauer disk diffusion method against Gram negative and Gram positive bacterial strains. Physicochemical properties of modified arabinoxylans were different from arabinoxylan yet were satisfactory for their use as pharmaceutical excipients.  Arabinoxylan showed strong antimicrobial activity against Gram positive strains.  However, it showed no antimicrobial activity against Gram negative strains. Carboxymethyl arabinoxylan showed maximum activity against<em> S. epidermidis</em>. It also showed activity against <em>S. aureus</em> and <em>P. aeruginosa</em>.  Arabinoxylan-Na showed concentration-dependent antimicrobial activity. This study provides the first report on the antibacterial properties of arabinoxylan and its modified forms.</p><p> </p>


2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Helmoz R. Appelt ◽  
Julieta S. Oliveira ◽  
Roberto C. V. Santos ◽  
Oscar E. D. Rodrigues ◽  
Maura Z. Santos ◽  
...  

A series of D-glucosamine derivatives were synthesized (2–4) and evaluated for their antimicrobial activity. Some of the compounds investigated have shown significant antimicrobial activity against Gram-positive and Gram-negative bacterial strains as well as a few fungal strains. The results suggest that the presence of sugar moiety is necessary to biological activity.


Author(s):  
Vaishnavi. P. Gilava ◽  
Dr. Praful. K. Patel

An effectual direct synthesis of 1,4-dihydropyrimido[1,2-a]benzimidazole (C-01 to C-10) was developed from 1H-benzo[d]imidazol-2-amine, 4-(benzyloxy)-3-methoxybenzaldehyde, N-(substituted phenyl)-3-oxobutanamide by adding few drop of DMF and in presence of conc.HCL. The product was obtained after about 5 hours of heating in refluxing condition. The synthesized compounds were characterized by different spectral and elemental analysis. Some of the obtained compounds showed a promising antimicrobial activity on screening against Gram-positive and Gram-negative bacterial strains.


2020 ◽  
Author(s):  
Nusrat Abedin ◽  
Abdullah Hamed A Alshehri ◽  
Ali M A Almughrbi ◽  
Olivia Moore ◽  
Sheikh Alyza ◽  
...  

Antimicrobial resistance (AMR) has become one of the more serious threats to the global health. The emergence of bacteria resistant to antimicrobial substances decreases the potencies of current antibiotics. Consequently, there is an urgent and growing need for the developing of new classes of antibiotics. Three prepared novel iron complexes have a broad-spectrum antimicrobial activity with minimum bactericidal concentration (MBC) values ranging from 3.5 to 10 mM and 3.5 to 40 mM against Gram-positive and Gram-negative bacteria with antimicrobial resistance phenotype, respectively. Time-kill studies and quantification of the extracellular DNA confirmed the bacteriolytic mode of action of the iron-halide compounds. Additionally, the novel complexes showed significant antibiofilm activity against the tested pathogenic bacterial strains at concentrations lower than the MBC. The cytotoxic effect of the complexes on different mammalian cell lines show sub-cytotoxic values at concentrations lower than the minimum bactericidal concentrations.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem

Substituted-6-methyl-1-thioxo-1,2-dihydro-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-ones (5a,b) were synthesized from condensation of visnagenone (2a) or khellinone (2b) with 6-amino-thiouracil (3) in dimethylformamide or refluxing of (4a) or (4b) in dimethylformamide. Hence, compounds (5a,b) were used as the starting materials for preparing many new heterocyclic compounds such as; furo[3,2-g]pyrimido[1,6-a]quinazoline (6a,b), furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazolinone (7a,b), substituted-benzylidene-furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazoline-3,5-dione (8a–f), 3-oxo-furo[3,2-g]pyrimido[1,6-a]quinazoline-pentane-2,4-dione (9a,b), 1-(pyrazole)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (10a,b), 2-(oxo or thioxo)-pyrimidine-furo[3,2-g]pyrimido[1,6-a]quinazolinone (11a–d), 1-(methylthio)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (12a,b), 1-(methyl-sulfonyl)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (13a,b) and 6-methyl-1-((piperazine) or morpholino)-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-one (14a–d). The structures of the prepared compounds were elucidated on the basis of spectral data (IR, 1H-NMR, 13C-NMR, MS) and elemental analysis. Antimicrobial activity was evaluated for the synthesized compounds against Gram-positive, Gram-negative bacteria and fungi. The new compounds, furothiazolo pyrimido quinazolines 8a–f and 11a–d displayed results excellent for growth inhibition of bacteria and fungi.


2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Hessa H. Al-Rasheed ◽  
Monirah Al Alshaikh ◽  
Jamal M. Khaled ◽  
Naiyf S. Alharbi ◽  
Ayman El-Faham

Novel series of 4,6-disubstituted-1,3,5-triazines containing hydrazone derivatives were synthesized employing ultrasonic irradiation and conventional heating. The ultrasonication gave the target products in higher yields and purity in shorter reaction time compared with the conventional method. IR, NMR (H 1 and C 13), elemental analysis, and LC-MS confirmed the structures of the new products. The antimicrobial and antifungal activities were evaluated for all the prepared compounds against some selected Gram-positive and Gram-negative bacterial strains. The results showed that only two compounds 7i (pyridine derivative) and 7k (4-chlorobenzaldehyde derivative) displayed biological activity against some Gram-positive and Gram-negative bacteria, while the rest of the tested compounds did not display any antifungal activity.


2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Shiara Ramdath ◽  
John Mellem ◽  
Londiwe Simphiwe Mbatha

Health issues involving inadequate treatment of diseases such as cancer and microbial infections continue to be the subject of much ongoing recent research. Biosynthesized silver nanoparticles (AgNPs) were characterized using Transmission Electron Microscopy (TEM), Zeta Sizer, Ultraviolet (UV), and Fourier Transform Infrared (FTIR) spectroscopy. Their antimicrobial activity was evaluated on selected Gram-positive and Gram-negative bacterial strains, using the disc diffusion and broth dilution assays. Cell viability profiles were evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and apoptosis studies on selected human noncancer and cancer cells. The biosynthesized AgNPs were evaluated to be spherical clusters, with sizes between 40 and 70 nm. The absorption peak at 423 nm and the presence of polyphenols confirmed the synthesis and stabilization of these tested AgNPs. The AgNPs showed a good stability of −23.9 ± 1.02 mV. Good antimicrobial activity (6.0–18.0 mm) was seen on all tested bacteria at a minimum inhibitory concentration (MIC) ranging from 5 to 16 μg/ml, with the highest activity seen against Gram-negative Escherichia coli (18 ± 0.5 mm), and the lowest activity was seen against Gram-positive Listeria monocytogenes (6.0 ± 0.4 mm) after treatment with the AgNPs. These NPs showed a concentration-dependent and cell-specific cytotoxicity with low IC50 values (41.7, 56.3, and 63.8 μg/ml). The NPs were well tolerated by tested cells as indicated by a more than 50% cell viability at the high dose tested and low apoptotic indices (<0.2). These findings indicated that these biosynthesized AgNPs showed great potential as effective antibacterial agents and anticancer drug delivery modalities.


2008 ◽  
Vol 73 (7) ◽  
pp. 683-690 ◽  
Author(s):  
Dipti Dodiya ◽  
Amit Trivedi ◽  
Samir Jarsania ◽  
Shailesh Vaghasia ◽  
Viresh Shah

The synthesis of substituted pyrazolo[3',4':4,5]thieno[2,3-d]pyrimidin-8-ones (IIIa-j) from 5-amino-3-methyl-1H-thieno[3,2-c]pyrazole-6-carbonitrile (II) is described. The key compound II was synthesized from (5-methyl- -2,4-dihydro-3H-pyrazol-3-ylidene)malononitrile I via the Gewald reaction. The synthesis of the title compounds IIIa-j was accomplished by condensation of II with different aromatic aldehydes. The newly synthesized heterocyles were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectroscopic investigation. All the newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains. .


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