Synthesis, antibacterial, and antifungal activities of new pyrimidinone derivatives

2015 ◽  
Vol 21 (4) ◽  
pp. 191-194 ◽  
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 ◽  
Antibacterial And Antifungal Activities ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal

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.

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

2015 ◽  
Vol 11 ◽  
pp. 869-874 ◽  
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 ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Derivatives ◽  
Antibacterial And Antifungal ◽  
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.

scholarly journals Antimicrobial Activity of Apple Cider Vinegar

2017 ◽  
Vol 16 (2) ◽  
pp. 11-15 ◽  
Author(s):  
Asma Saqib
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Medicinal Purpose ◽  
Diverse Range ◽  
Antifungal Activities ◽  
Apple Cider ◽  
Antibacterial And Antifungal Activities ◽  
Medicinal Properties ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal

In recent years, there has been a growing interest in researching and developing new antimicrobial agents from various sources to combat microbial resistance. Apple cider vinegar, otherwise known as cider vinegar or ACV, is a type of vinegar made from cider or apple must and has a pale to medium amber color. Unpasteurized or organic ACV contains mother of vinegar. It has been used for medicinal purpose for thousands of years for its various medicinal properties. The antimicrobial activity of cider vinegar has been recognized but not investigated. It can be used as alternative to commercial antimicrobial agents. The present study aims at finding the antibacterial and antifungal activities of various dilutions of ACV against diverse range of bacteria and fungi to generate data for which little investigation exist.

scholarly journals Synthesis, Characterization and Biological Evaluation of some Novel Pyrazolo[1,5-a]Pyrimidine Derivatives

2016 ◽  
Vol 65 ◽  
pp. 11-26
Author(s):  
Nilesh M. Thumar ◽  
Ankur A. Kaneria ◽  
Milan Vadodaria ◽  
Kartik Ladva
Keyword(s):  
Antimicrobial Activity ◽  
Broad Spectrum ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Pyrimidine Derivatives ◽  
Gram Negative ◽  
H Nmr ◽  
Ketene Dithioacetals ◽  
Convenient Synthesis ◽  
Bacteria And Fungi

A convenient synthesis of substituted Pyrazolo[1,5-a]pyrimidine was carried out by the reaction of different ketene dithioacetals with different aromatic amine in isopropanol in the presence of potassium carbonate. The newly synthesized compound were characterized by1H NMR, IR, Mass and screened for their antimicrobial activity against various strains of bacteria and fungi. From the synthesized different NCEs, compounds 8a, 8d and 8e are broad spectrum drug which can inhibit the growth of gram positive, gram negative bacteria and fungi.

scholarly journals Screening of various solvents and extracts of Achillea latiloba Ledeb. ex Nordm for antibacterial and antifungal activities

2014 ◽  
Vol 60 (2) ◽  
pp. 29-40 ◽  
Author(s):  
Ömer Ertürk
Keyword(s):  
Streptococcus Mutans ◽  
Salmonella Enteritidis ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Gram Positive ◽  
Gram Negative ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal

Abstract In this study the antibacterial and antifungal activities of extracted Achillea latiloba Ledeb. ex Nordm (Asteraceae) samples in acetone, ethyl acetate, ethanol, methanol and dimethyl sulfoxide (DMSO) from Trabzon Province (Turkey) were investigated. Antimicrobial activity of A. latiloba varied depending on the extract of samples, dosage of extracts, and the extraction solvents for all test microorganisms. Staphylococcus aureus, Streptococcus salivarius, Klebsiella pneumoniae, Escherichia coli, Salmonella enteritidis, Streptococcus pneumoniae, Bacillus cereus, Listeria monocytogenes, Streptococcus mutans, Pseudomonas aeruginosa, Bacillus licheniformis, Micrococcus luteus, Bacillus subtillis, Proteus vulgaris and Candida albicans were studied with use of disc diffusion and agar dilution method. The results indicated that each of the crude extracts of Achillea latiloba exhibited a more or less pronounced antibacterial and antifungal potency both in Gram-positive and Gram-negative bacteria and fungi. While in the Gram-negative group, the most sensitive microorganism to Achillea latiloba were S. enteritidis and Streptococcus mutans which is Gram-positive. In the Gram-positive group, the microorganisms most sensitive to Achillea latiloba were Streptococcus mutans and L. monocytogenes. However, the least sensitive microorganism was P. vulgaris. The results presented in this paper suggest that Achillea latiloba possesses additional antimicrobial activities that has an effect against some Gram-negative, Gram-positive bacteria and fungi.

Evaluation of topologically distinct constrained antimicrobial peptides with broad-spectrum antimicrobial activity

2018 ◽  
Vol 16 (32) ◽  
pp. 5764-5770 ◽  
Author(s):  
Fang Yuan ◽  
Yuan Tian ◽  
Weirong Qin ◽  
Jingxu Li ◽  
Dan Yang ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Peptides ◽  
Microbial Activity ◽  
Broad Spectrum ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Conformationally Constrained ◽  
Constrained Peptides ◽  
Hydrophilic Residues ◽  
Bacteria And Fungi

Conformationally constrained peptides with either α-helical or β-hairpin conformations, possessing different topological distribution of hydrophobic and hydrophilic residues, displayed distinct anti-microbial activity towards Gram positive and Gram negative bacteria and fungi.

scholarly journals Chemical Composition and Antimicrobial Activity of the Essential Oil from Flowers of Eryngium triquetrum (Apiaceae) Collected Wild in Sicily

2016 ◽  
Vol 11 (7) ◽  
pp. 1934578X1601100
Author(s):  
Simona Casiglia ◽  
Maurizio Bruno ◽  
Sergio Rosselli ◽  
Felice Senatore
Keyword(s):  
Antimicrobial Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Art Works ◽  
Main Components ◽  
Antibacterial And Antifungal ◽  
Historical Art

The chemical composition of the essential oil from flowers of Eringium triquetrum Vahl. collected in Sicily was evaluated by GC and GC-MS. The main components were pulegone (50.6%), piperitenone (30.5%) and menthone (7.0%). Comparison of this oil with other studied oils of Eringium species is discussed. The oil showed good antibacterial and antifungal activities against some microorganisms that infest historical art works.

scholarly journals Synthesis of New Furothiazolo Pyrimido Quinazolinones from Visnagenone or Khellinone and Antimicrobial Activity

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem
Keyword(s):  
Antimicrobial Activity ◽  
Growth Inhibition ◽  
Spectral Data ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Heterocyclic Compounds ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Bacteria And Fungi ◽  
New Compounds

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.

scholarly journals Synthesis, characterization, and evaluation of antioxidant and antimicrobial activity of three novel n-heteroaromatic hydrazonyl-thiazoles

2021 ◽  
Vol 10 (2) ◽  
pp. 14-23
Author(s):  
Sanja Kokanov ◽  
Milan Nikolić ◽  
Irena Novaković ◽  
Tamara Todorović ◽  
Nenad Filipović
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Antimicrobial Activity ◽  
Antioxidative Activity ◽  
Drug Candidate ◽  
Resonance Spectroscopy ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Antioxidant And Antimicrobial Activity ◽  
Bacteria And Fungi ◽  
Approved Drugs

(Thiazolyl-2-yl)hydrazones (THs) are a group of organic compounds containing both hydrazone and 1,3-thiazole pharmacophores present in many approved drugs. They have been investigated greatly in recent years due to potent anticancer, antibacterial, antifungal, antituberculosis, anti-inflammatory, and antiparasitic activities. In this study, one pyridine-based and two quinoline-based, novel THs were synthesized and characterized by elemental analysis, Fourier-transform infrared spectroscopy (FTIR), and nuclear magnetic resonance spectroscopy (NMR). The antimicrobial activity of the compounds was tested against five Gram-positive and five Gram-negative bacteria, as well as against three fungi. The antioxidant capacity of the compounds was tested in six antioxidative assays. The results showed that quinoline-based THs were more active against tested Gram-negative bacteria and fungi strains than pyridine-based compounds. All the compounds showed excellent antioxidative activity comparable to or greater than the used standards (vitamin C and Trolox). Absorption, distribution, metabolism, excretion, and toxicity (ADMET) parameters were calculated in-silico. Results pointed to promising good pharmacokinetics profiles of investigated compounds, especially 2-quinoline carboxaldehyde-based compound, which can be a lead drug candidate.

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

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Serkan Yavuz ◽  
Hilal Yıldırım
Keyword(s):  
Inhibitory Concentration ◽  
Antibacterial Activities ◽  
Klebsiella Pneumonia ◽  
Gram Negative Bacteria ◽  
Ferrocene Derivatives ◽  
Antifungal Activities ◽  
Gram Positive Bacteria ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Antibacterial And Antifungal

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.

scholarly journals Synthesis and Antimicrobial Assessment of Fe3+ Inclusion Complex of p-tert-Butylcalix[4]arene Diamide Derivative

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Anwar Ali Chandio ◽  
Ayaz Ali Memon ◽  
Shahabuddin Memon ◽  
Fakhar N. Memon ◽  
Qadeer Khan Panhwar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Gram Negative ◽  
Mueller Hinton ◽  
Mueller Hinton Agar ◽  
Ft Ir ◽  
Bacteria And Fungi

Present study deals with the synthesis of the p-tert-butylcalix[4]arene diamide derivative as ligand (L) and its Fe3+ complex, followed by its characterization using TLC and FT-IR, while UV-Vis and Job’s plot study were performed for complex formation. Antimicrobial activity of the derivative (L) and its metal complex was carried out by the disc diffusion method against bacteria (Escherichia coli and Staphylococcus albus) and fungi (R. stolonifer). Different concentrations of the derivative (L) (6, 3, 1.5, 0.75, and 0.37 μg/mL) and its Fe3+ complex were prepared, and Mueller–Hinton agar was used as the medium for the growth of microorganisms. Six successive dilutions of the derivative (L) and Fe3+ complex were used against microorganisms. Two successive dilutions (6 and 3 μg/mL) of the derivative (L) showed antibacterial action against both Gram-positive and Gram-negative bacteria. In addition, three successive dilutions (6, 3, and 1.5 μg/mL) of the derivative (L) showed antifungal activity. However, all of six dilutions of the Fe3+ complex showed antimicrobial activity. Derivative (L) showed 3 and 1.5 μg/mL minimum inhibitory concentrations (MIC) against bacteria and fungi, respectively. On the contrary, its Fe3+ complex showed 0.37 μg/mL value of MIC against bacteria and fungi. Hence, Fe3+ complex of the derivative (L) was found to be a more effective antimicrobial agent against selected bacteria and fungi than the diamide derivative (L).

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