Synthesis of 1,5-disubstituted 1,2,3-triazole via multi-component reaction

Magnetic Resonance Spectroscopic Analysis ◽

Resolution Mass

1,5-Disubstituted 1,2,3-triazoles are synthesized viametal-free multi-component reaction from primary amine, ketones and 4-nitrophenyl azide. The structure of three target compounds including:1-(4-methoxybenzyl)-5-(4-methylphenyl)-1H-1,2,3-triazole (1), 1-(4-methoxybenzyl)-5-(4-nitrophenyl)-1H-1,2,3-triazole (2) and 1-(4-methoxybenzyl)-5-phenyl-1H-1,2,3-triazole (3) is elucidated and identified by infrared spectroscopy, nuclear magnetic resonance spectroscopic analysis and high resolution mass spectrum. The formation of heterocyclic aromatic 1,2,3-triazole ring is approved by the appearance of singlet peak at 7.71 ppm in 1H NMR corresponding with triazolyl proton. In addition, antibacterial and antifungal activities of products are also tested with three Gram-positive bacteria (B. subtilis, S. aureus and L. fermentum), three Gram-negative bacteria (P. aeruginosa, E.coli, S. enterica), and Candida albicans fungus.

Synthesis and Biological Evaluation of some Novel Pyrano[2,3-d]Pyrimidine Derivatives

International Letters of Chemistry Physics and Astronomy ◽

10.18052/www.scipress.com/ilcpa.74.9 ◽

2017 ◽

Vol 74 ◽

pp. 9-14

Author(s):

Pratik K. Talpara ◽

Guarang G. Dubal ◽

Viresh H. Shah

Keyword(s):

Biological Evaluation ◽

Alder Reaction ◽

Gram Negative Bacteria ◽

Pyrimidine Derivatives ◽

Gram Positive ◽

Gram Negative ◽

Gram Positive Bacteria ◽

The synthesis of novel Pyrano[2,3-d]pyrimidine derivatives, had been synthesized by three component domino Knoevenagel hetero Diels-Alder reaction. The products were assayed for their in vitro biological assay antibacterial activity against with two Gram-positive bacteria Staphylococcus aureus MTCC-96, Streptococcus pyogenes MTCC 443, two Gram-negative bacteria Escherichia coli MTCC 442, Pseudomonas aeruginosa MTCC 441 and three fungal strains Candida albicans MTCC 227, Aspergillus Niger MTCC 282, Aspergillus clavatus MTCC 1323 taking ampicillin, chloramphenicol, ciprofloxacin, norfloxacin, nystatin, and griseofulvin as standard drugs. Among the various synthesized heterocyclic compounds, 1b, 1c and 1g are display broad spectrum antibacterial and antifungal activities against both gram-positive and gram-negative bacteria as compared with standard drugs.

N-Alkyl derivatives of diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside; synthesis and antimicrobial activity

Beilstein Journal of Organic Chemistry ◽

10.3762/bjoc.11.97 ◽

2015 ◽

Vol 11 ◽

pp. 869-874 ◽

Cited By ~ 11

Author(s):

Agata Walczewska ◽

Daria Grzywacz ◽

Dorota Bednarczyk ◽

Małgorzata Dawgul ◽

Andrzej Nowacki ◽

...

Keyword(s):

Antimicrobial Activity ◽

Pathogenic Fungi ◽

Pharmacological Properties ◽

Gram Negative Bacteria ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Alkyl Derivatives ◽

Derivatives Of

Diosgenyl 2-amino-2-deoxy-β-D-glucopyranoside is a synthetic saponin exhibiting attractive pharmacological properties. Different pathways tested by us to obtain this glycoside are summarized here. Moreover, the synthesis of N-alkyl and N,N-dialkyl derivatives of the glucopyranoside is presented. Evaluation of antibacterial and antifungal activities of these derivatives indicates that they have no inhibitory activity against Gram-negative bacteria, whereas many of the tested N-alkyl saponins were found to inhibit the growth of Gram-positive bacteria and human pathogenic fungi.

SYNTHESIS, CHARACTERIZATION, AND ANTIMICROBIAL EVALUATION OF NEW N-PHENYLCINNAMAMIDE DERIVATIVES LINKED TO ASPIRIN AND IBUPROFEN

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i10.26937 ◽

2018 ◽

Vol 11 (10) ◽

pp. 443

Author(s):

Ameer H Alwash ◽

Alaa M Mahdi ◽

Haider J Al-karagully

Keyword(s):

Ethyl Chloroformate ◽

Resonance Spectroscopy ◽

Gram Negative Bacteria ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Antimicrobial Evaluation ◽

Ester Linkage ◽

Different Strains ◽

Antibacterial Evaluation

Objective: The objective of this study was to synthesize phenylcinnamamide (substituted acetanilide chalcone) derivatives linked to aspirin and ibuprofen with potential antibacterial and antifungal activity.Methods: Substituted acetanilide compounds were reacted with different arylaldehydes through Claisen-Schmidt condensation in the presence of KOH. They formed differently substituted acetanilide chalcones (1a-e) which are linked to aspirin and ibuprofen through an ester linkage to form compounds (2a-j) using ethyl chloroformate (ECF) as a catalyst.Results: The synthesized compounds have been characterized by elemental analysis, Fourier transform infrared and1H-nuclear magnetic resonance spectroscopy. An antibacterial evaluation was achieved for Gram-positive bacteria (Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli) and antifungal for Candida albicans.Conclusion: Compounds (2a-j) have shown intermediate antimicrobial activity against different strains of microorganisms.

Ferrocene Derivatives Carrying Urea, Thiourea, and Sulfonamide Moieties: Synthesis and Evaluation of Antibacterial and Antifungal Activities

Journal of Chemistry ◽

10.1155/2013/149693 ◽

2013 ◽

Vol 2013 ◽

pp. 1-7 ◽

Cited By ~ 8

Author(s):

Serkan Yavuz ◽

Hilal Yıldırım

Keyword(s):

Inhibitory Concentration ◽

Antibacterial Activities ◽

Klebsiella Pneumonia ◽

Gram Negative Bacteria ◽

Ferrocene Derivatives ◽

Antifungal Activities ◽

Gram Positive Bacteria ◽

Elemental Analyses ◽

In the present study, some novel ferrocene derivatives carrying urea, thiourea, and sulfonamide groups were synthesized, and all compounds were characterized by spectral and elemental analyses. These compounds were screened for their antibacterial activities and also their minimum inhibitory concentration (MIC) against Gram-positive bacteria (Staphylococcus aureusandBacillus subtilis) and Gram-negative bacteria (Klebsiella pneumoniaandEscherichia coli) and antifungal activities againstSaccharomyces cerevisiaeandCandida albicans. Amongst the tested compounds,4b,4c,5b, and6bdisplayed excellent antimicrobial activity.

Synthesis, antibacterial, and antifungal activities of new pyrimidinone derivatives

Heterocyclic Communications ◽

10.1515/hc-2015-0066 ◽

2015 ◽

Vol 21 (4) ◽

pp. 191-194 ◽

Cited By ~ 5

Author(s):

Oussama Cherif ◽

Fatma Masmoudi ◽

Fatma Allouche ◽

Fakher Chabchoub ◽

Mohamed Trigui

Keyword(s):

Antimicrobial Activity ◽

Broad Spectrum ◽

Pathogenic Fungi ◽

Gram Negative Bacteria ◽

Efficient Synthesis ◽

Gram Negative ◽

Antifungal Activities ◽

Bacteria And Fungi ◽

AbstractAn efficient synthesis of new pyrrolopyrimidinones 3a-d and isoxazolopyrimidinones 4a-c from the respective aminocyanopyrroles 1a-d and aminocyanoisoxazoles 2a-c is presented. The synthesized compounds were screened for antimicrobial activity against a panel of bacteria and fungi. Compound 4c exhibits remarkable activity against a broad spectrum of Gram-positive and Gram-negative bacteria and pathogenic fungi.

Antimicrobial Evaluation of Leaf and Stem Extract of Cordia macleodii

Open Pharmaceutical Sciences Journal ◽

10.2174/1874844901401010001 ◽

2014 ◽

Vol 1 (1) ◽

pp. 1-3 ◽

Cited By ~ 3

Author(s):

Deepkumar Joshi ◽

Rinku Patel ◽

Nupur Patel ◽

Devendra Patel ◽

Chintan Pandya

Keyword(s):

Antimicrobial Activities ◽

Maximum Amount ◽

Gram Negative Bacteria ◽

Gram Negative ◽

E Coli ◽

Gram Positive Bacteria ◽

Antifungal Potential ◽

Stem Extract ◽

Antimicrobial Evaluation ◽

The leaf and stem of cordia macleodii plant were investigated for evaluating antibacterial and antifungal properties.Different extracts of leaf and stem viz. double distilled water, methanol, ethyl acetate ane n-hexane were collectedand content was optimized for the maximum amount of extraction with varying time of 6 and 12 h. The extracts weretested for their antimicrobial activities against gram-positive bacteria (B. sutilis), gram-negative bacteria (E. coli) andfungi (A. niger). The extracts were found to be more active against bacteria as compared to fungi. It was also observedthat the antibacterial and antifungal potential of the water extracts were found to be excellent as 1A (38 mm) and 1B (22mm) compared to the other extracts. Graphical Abstract:

Design, Synthesis and Antimicrobial Activity of Some Triazine Chalcone Derivatives

Anti-Infective Agents ◽

10.2174/2211352517666190710115111 ◽

2021 ◽

Vol 18 (4) ◽

pp. 332-338

Author(s):

Ravindra Sandipan Shinde ◽

Satish Ashruba Dake ◽

Rajendra Pundalikrao Pawar

Keyword(s):

Escherichia Coli ◽

Candida Glabrata ◽

Gram Negative Bacteria ◽

Antibacterial And Antifungal Activity ◽

Design Synthesis ◽

Gram Negative ◽

Chalcone Derivatives ◽

Gram Positive Bacteria ◽

Target Molecules ◽

Background: A series of Triazine Chalcone derivatives were synthesized by the condensation of 1-(4-((4,6-dimethoxy-1,3,5-triazin-2-yl)amino)phenyl)ethanone with substituted benzaldehyde in methanol solvent. Methods: All the synthesized derivatives (3a-l) were screened for their anti-bacterial evaluation against Gram negative bacteria Escherichia coli (NCIM 2137) and Pseudomonas aeruginosa (NCIM 2036); Gram positive bacteria Staphylococcus aureus, Bacillus subtilis (NCIM 2250) and four fungal stains. Candida albicans (MTCC 227), Aspergillus niger (NCIM 545), Candida tropicalis (NCIM 3110) and Candida glabrata (NCIM 3236). Results and Conclusion: Several target molecules throughout the series showed good antibacterial and antifungal activity against tested stains.

Intracellular and Extracellular extracts activity of Oscillatoria limnetica and Chroococus minor against some Bacteria and Fangi

Baghdad Science Journal ◽

10.21123/bsj.8.1.478-483 ◽

2011 ◽

Vol 8 (1) ◽

pp. 478-483

Author(s):

Baghdad Science Journal

Keyword(s):

Culture Media ◽

Inhibition Zone ◽

Antagonistic Activity ◽

Diffusion Method ◽

Gram Negative Bacteria ◽

Gram Positive ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Extracellular Products ◽

In this study Oscillatoria limnetica and Chroococus minor were isolated ?purified and identification from water canal around Baghdad University Campus. The water of this canals originally from Tigris River. BG-11 culture media was used for their cultivation in suitable laboratory conditions (25c°, 200µE/m2/sec) for 16:8 hrs. Light: dark. Each culture was harvested at the end of exponential phase .Organic solvents used for extraction were Ethanol? Hexane and Methanol 95% to extract the crude active Intracellular and Extracellular substances, and evaporated down to dryness .Antibacterial and antifungal activity of these different extracts were evaluated against 6 strains of gram positive bacteria and gram negative bacteria in addition to fungi, Agar diffusion method was used in this evaluation. Results showed that the extracellular products which extracted by hexane and the extracellular products which extracted by ethanol from Oscillatoria limnetica were have higher antagonistic activity against bacteria and Fungi comparing with methanol extracts .However higher antibacterial and antifungal were obtained against the studied strains of comparing with methanol and ethanol extracts of the same algae products. The gram positive bacteria studied revealed higher susceptibility to attack by the intracellular and extracellular extracts comparing with the gram negative bacteria. These extracts revealed higher antibacterial activity against Bacillus subtilise and the average of inhibition zone were 26, 22 mm. for intracellular and extracellular products of O.limnetica respectively. However, C. minor intracellular products extract has the antagonistic activity against Staphylococcus aureus with 28 mm inhibition zone

Antibacterial Activity of New Compounds Based on Nanocomposites

Avicenna Journal of Clinical Microbiology and Infection ◽

10.34172/ajcmi.2021.17 ◽

2021 ◽

Vol 8 (3) ◽

pp. 94-97

Author(s):

Maryam Kouhkan ◽

Fatemeh Ghanbary ◽

Fatemeh Karimi

Keyword(s):

Titanium Dioxide ◽

Titanium Dioxide Nanoparticles ◽

Sol Gel ◽

Preliminary Evaluation ◽

Gram Negative Bacteria ◽

Gram Negative ◽

Gram Positive Bacteria ◽

Agar Dilution ◽

New Compounds

Background: Antimicrobial resistance is a major problem in treatment and public health, and it has been increasing over the last few decades. Hence, serious measurements are needed to overcome this challenge. In this study, we evaluated antibacterial and antifungal activity of some nanocomposites including titanium dioxide (5a), polyimide nanocomposites containing cerium oxide (5b), silver-titanium dioxide nanoparticles prepared under desired conditions (5c), polyaniline/wheat husk ash PANI /WHA (5d), Ag-TiO2 prepared by sol–gel route (5e), and cellulose-graphene (5f) against some bacterial and fungal strains, which are the most common agents in many infectious diseases. Methods: The nanoparticles were prepared in desired condition. The agar dilution and well agar diffusion methods were used for determination of inhibition zoon and minimum inhibitory concentration (MIC) during preliminary evaluation of antimicrobial activity against Staphylococcus aureus, Streptococcus pyogenes, Pseudomonas aeruginosa, Escherichia coli and Candida albicans. Results: The results showed that the nanocomposites had good activity against gram-negative bacteria. Conclusions: Our results showed that the inhibitory activity of these nanocomposites on gram-negative bacteria was better than gram-positive bacteria.

Rapid demonstration of septic or infectious arthritis due to Gram-negative bacteria

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100123830 ◽

1992 ◽

Vol 50 (1) ◽

pp. 686-687

Author(s):

Jacob S. Hanker ◽

Paul R. Gross ◽

Beverly L. Giammara

Keyword(s):

Chronic Arthritis ◽

Blood Cultures ◽

Gram Negative Bacteria ◽

Infectious Arthritis ◽

Bacterial Arthritis ◽

Gram Positive ◽

Gram Negative ◽

Gram Positive Bacteria

Blood cultures are positive in approximately only 50 per cent of the patients with nongonococcal bacterial infectious arthritis and about 20 per cent of those with gonococcal arthritis. But the concept that gram-negative bacteria could be involved even in chronic arthritis is well-supported. Gram stains are more definitive in staphylococcal arthritis caused by gram-positive bacteria than in bacterial arthritis due to gram-negative bacteria. In the latter situation where gram-negative bacilli are the problem, Gram stains are helpful for 50% of the patients; they are only helpful for 25% of the patients, however, where gram-negative gonococci are the problem. In arthritis due to gram-positive Staphylococci. Gramstained smears are positive for 75% of the patients.