Synthesis of Some New Derivatives of Pyrrolidine-2-one and Studying Their Antibacterial Potentials

2020 ◽  
Vol 38 (3B) ◽  
pp. 128-141
Author(s):  
Nadia A. Betti ◽  
Redha Ib. Hussain ◽  
Sahar Ab. Kadhem
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Mass Spectra ◽  
Biological Activities ◽  
Ft Ir ◽  
Derivatives Of ◽  
And Staphylococcus Aureus

New derivatives of pyrrolidine-2-one have been synthesized through lactamization of γ –butyrolactone (GBL) by hydrazine hydrate (80%), ethylene diamine and ethanol amine to afford compounds (1-aminopyrrolidin-2-one), (1-(2-aminoethyl)pyrrolidine-2-one) and (1-(2-hydroxyethyl)pyrrolidine-2-one), respectively. Compound (1-aminopyrrolidin-2-one) underwent several reactions to synthesize the rest of these derivatives. All synthesized compounds were approved by their FT-IR, 1H-NMR and some by Mass spectra. The biological activities of these derivatives were evaluated against Escherichia coli and Staphylococcus aureus. Many of these derivatives showed moderate biological activity against one or both kind of bacteria in comparison to amoxicillin and some showed no biological activity at all.

scholarly journals Synthesis , Characterization and Study of Biological Activity of Some New Schiff Bases ,1,3-Oxazepine and Tetrazole Derived from 2,2 di thiophenyl Acetic Acid

2018 ◽  
Vol 31 (1) ◽  
pp. 189 ◽  
Author(s):  
Eman M. Hussain ◽  
Hussam Z. Naji
Keyword(s):  
Mass Spectrometry ◽  
Staphylococcus Aureus ◽  
Acetic Acid ◽  
Biological Activity ◽  
Hydrazine Hydrate ◽  
Schiff Bases ◽  
Sodium Azide ◽  
Derivatives Of ◽  
Tetrazole Derivatives ◽  
And Staphylococcus Aureus

         In this study  new  derivatives  of  Schiff bases 5-8 , 1,3- oxazepine  9-16 and tetrazoles 17-19 have  been synthesized from the new starting  material 1 which has  synthesized  the reaction of  one mole of dichloro acetic acid and two moles of  thiophenol , the esters  2-3 were synthesized from the reaction of  compound 1 with methanol or ethanol respectively  in the presence of  H2SO4  as  catalyst  then 2,2-dithiophenylaceto Hydrazide  4 were synthesized from the reaction of  2 or 3 with hydrazine hydrate  80 % , Schiff bases 5-8 were  synthesized from the reaction of  4 with appropriate aldehyde or ketone .Treatment  of  Schiff bases with maleic and phathalic  anhydride in dry benzene to give 1,3-oxazepen derivatives  9-16 and with sodium azide in tetrahydrofuran (THF) afforded  tetrazole derivatives 17-19. All these compounds have been characterized from their melting pointes, FTIR , 1HNMR and compounds 1,5 and 18 by mass spectrometry . Derivatives 6,7,11,16,17 and 18 were tested against inhibition of E.coli and. Staphylococcus- aureus and were all funds to be active. Scheme (1).

Study on Propolis Quality from China and Uruguay

2000 ◽  
Vol 55 (9-10) ◽  
pp. 778-784 ◽  
Author(s):  
Josep Serra Bonvehí ◽  
Francesc Ventura Coll
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Biological Activities ◽  
The State ◽  
Active Components ◽  
E Coli ◽  
Geographic Origins ◽  
Potential Activity ◽  
And Staphylococcus Aureus

Abstract The composition, bacteriostatic and ROO• -scavenging potential activities of fifteen propolis samples from various botanic and geographic origins were determined to obtain objective information related to propolis quality. Variance analysis showed significant differences (p ≤ 0.05) in the contents of polyphenols, flavonoids and active components between fresh and aged propolis. The state of the product (fresh or aged) could be differentiate by using flavonoid pattern and biological activities. A minimum propolis concentration of 80 μg/ml was required inhibit Bacillus subtilis and Staphylococcus aureus while 800 μg/ml was required to inhibit Escherichia coli using fresh propolis. Aged propolis inhibit B. subtilis and S. aureus at concentration of 100 μg/ml and E. coli at 1000 μg/ml. A minimum flavonoids percentage of 18 g/100 g and a maximum ROO• -scavenging potential activity of 4.3 μg/ml were determined in fresh propolis. Flavonoids levels in aged propolis were approximately 20% lower than in fresh propolis. A maximum flavonoids percentage of 19.8 g/100 g and a ROO•-scavenging potential activity between 5.7 to 6.4 μg/ml in aged propolis were quantified. Another objective was to assess the use of ROO•-scavenging potential activity in propolis quality.

scholarly journals The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

2021 ◽  
Vol 90 (1) ◽  
pp. 2
Author(s):  
Halyna Hryhoriv ◽  
Illia Mariutsa ◽  
Sergiy M. Kovalenko ◽  
Victoriya Georgiyants ◽  
Lina Perekhoda ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Antibacterial Agents ◽  
Docking Studies ◽  
Synthetic Method ◽  
Bacillus Subtilis Atcc ◽  
Resistant Strains ◽  
Derivatives Of

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.

scholarly journals Preparation, Characterization, Biological Evaluation and Assess Laser Efficacy for New Derivatives of Imidazolidin-4-one

2021 ◽  
pp. 41-51
Author(s):  
Adil Hussein Dalaf ◽  
Fawzi Hameed Jumaa ◽  
Hanaa Kaain Salih
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Staphylococcus Epidermidis ◽  
Traditional Method ◽  
Biological Evaluation ◽  
Klebsiella Pneumonia ◽  
Microwave Method ◽  
Microwave Technology ◽  
Ft Ir ◽  
Derivatives Of

In this study, new Imidazolidin-4-one [A1-A5] compounds were prepared by the reaction of schiff base compounds with alanine in ethanol. The prepared compounds were characterized by physical properties, UV-Vis, FT-IR and 1H-NMR spectral and C.H.N analysis. TLC checked the purity for these compounds. All compounds [A1-A5] were prepared by the traditional method (reflux) and microwave technology. It was found that using the microwave method gives better results in terms of less time and, higher yield. Antibacterial behaviors were investigated against a variety of bacteria, including Escherichia coli and Klebsiella pneumonia Gram (-) ve, Staphylococcus aureus, and Staphylococcus epidermidis Gram (+) ve. The laser efficacy of the compounds [A1-A5] was evaluated after they were radiated by laser for (10, 20, 30) seconds. As the melting point and color of the substances were determined, it was discovered that they were unaffected and did not disintegrate or polymerize. Using the Chem Draw Specialist 19.0 program, the stereoisomers of the prepared compounds [A1-A5] were examined at the lowest layer stage. Using the Chem3D 19.0 program, the heat of the formulation of the compounds [A1-A5] was also investigated.

Microwave Assisted Synthesis and Antibacterial Evaluation of 1, 3, 4-Thiadiazole Derivatives

2021 ◽  
pp. 5293-5296
Author(s):  
Jayalakshmi P M ◽  
Sheeba Jasmin TS ◽  
Manu Jose
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
New Drugs ◽  
Diffusion Method ◽  
Microwave Assisted Synthesis ◽  
Ir And Nmr Spectroscopy ◽  
Analgesic Agents ◽  
Ft Ir ◽  
And Staphylococcus Aureus ◽  
Heterocyclic Moiety

1,3,4-Thiadiazole is an important heterocyclic moiety, forms an integral core structural component of different categories of drugs such as antimicrobial, antitubercular, anti-inflammatory, antiepileptic, antiviral, antineoplastics, and analgesic agents. It is a key moiety in current discovery and designing of new drugs. The compounds were synthesised by both conventional method and microwave method. The targeted derivatives can be synthesised in a shorter time under microwave condition than under conventional reaction condition. Their structures were confirmed by FT-IR and NMR Spectroscopy. Antibacterial property of two synthesised analogs were evaluated by Agar well diffusion method against Escherichia coli and Staphylococcus aureus. The results of antibacterial activity showed that both the compounds were active against Staphylococcus aureus and inactive against Escherichia coli. Results of invitro studies showed that modifications in SB-2-PHB and SB-8-PHB will make it as a promising lead molecule for further research.

scholarly journals Synthesis and Characterization of New Compounds Derived from Pyrrolidine-2-One and Evaluation of their Biological Activities

2020 ◽  
Vol 23 (4) ◽  
pp. 5-12
Author(s):  
Nadia A. Betti ◽  
◽  
Redha Ib. Hussain ◽  
Sahar Ab. Kadhem ◽  
Abdul Jabar Kh. Atia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Mass Spectrum ◽  
Biological Activities ◽  
The Other ◽  
Synthesis And Characterization ◽  
E Coli ◽  
Ft Ir ◽  
New Compounds ◽  
Derivatives Of

New derivatives of pyrrolidine-2-one have been prepared by lactamization of -butyrolactone GBL with hydrazine hydrate (NH2NH2(80%)) to afford (1-aminopyrrolidin-2-one) which undergo many reactions to prepare the other derivatives. The prepared derivatives were determined by utilizing their FT-IR,1H-NMR and some by Mass spectrum. These derivatives were evaluated biologically against (Staphylococcus aureusand E. coli).Some of these derivatives exhibited good biological activity against one or both kind of bacteria while some exhibited no biological activity at all.

Synthesis and Biological Activities of Chalcones Derived from Nitroacetophenone

2012 ◽  
Vol 518-523 ◽  
pp. 255-260 ◽  
Author(s):  
Xiao Yang Qiu ◽  
Su Zhi Li ◽  
An Ran Shi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Trichophyton Rubrum ◽  
Biological Activities ◽  
Tumor Cell Line ◽  
And Staphylococcus Aureus

A series of nitrochalcones (compounds 1-10) were synthesized by reacting appropriate nitroacetophenones and suitable benzaldehydes. The synthesized products were evaluated for their cytotoxic, antibacterial (Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence and Staphylococcus aureus) and antifungal (Aspergillus niger, Candida albicans and Trichophyton rubrum) activities in vitro. Among the compounds tested, (E)-3-(4-fluorophenyl)-1-(3-nitrophenyl)- prop-2-en-1-one (10) showed the favorable in vitro cytotoxic activity against human nasopharyngeal epidermoid tumor cell line KB, and (E)-3-(2-methoxyphenyl)-1-(3-nitrophenyl)prop-2-en-1-one (8) showed the strongest antimicrobial activity with MIC of 20 μg/mL against P. fluorescence.

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