scholarly journals Chemical Hydrogels Bearing Thiazolium Groups with a Broad Spectrum of Antimicrobial Behavior

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 2853 ◽  
Author(s):  
Alexandra Muñoz-Bonilla ◽  
Jakub Zagora ◽  
Daniela Plachá ◽  
Coro Echeverría ◽  
Alberto Chiloeches ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Water Solution ◽  
Thermal Polymerization ◽  
Inert Atmosphere ◽  
Gram Negative Bacteria ◽  
Monomer Content ◽  
Bacteria And Fungi ◽  
Thermal Stability Of ◽  
Potential Antimicrobial Activity ◽  
Positively Charged

Several hydrogels based on 2-hydroxyethyl methacrylate and a methacrylic monomer containing a thiazole group in its lateral chain have been prepared by thermal polymerization at 60 °C in water solution varying the chemical composition of the gels. The posterior quaternization of the thiazole groups with methyl iodine has rendered positively charged hydrogels with potential antimicrobial activity. This modification has been structurally characterized by infrared spectroscopy, whereas the thermal stability of all hydrogels has been studied by thermal degradation in inert atmosphere. The swelling behavior in distilled water and the rheology of the different hydrogels have been analyzed as a function of 2-(4-methylthiazol-5-yl)ethyl methacrylate (MTA) monomer content as well as its methylation. Finally, the active character of hydrogels against Gram-positive and Gram-negative bacteria and fungi has been evaluated, revealing excellent antimicrobial activity against all tested microorganisms. The methylated hydrogels could be used as potential materials for wound healing or contact lens applications.

scholarly journals Plant antimicrobial peptides: structures, functions, and applications

2021 ◽  
Vol 62 (1) ◽  
Author(s):  
Junpeng Li ◽  
Shuping Hu ◽  
Wei Jian ◽  
Chengjian Xie ◽  
Xingyong Yang
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Peptides ◽  
Agricultural Production ◽  
Food Additives ◽  
Antimicrobial Activities ◽  
Gram Positive Bacteria ◽  
Potential Applications ◽  
Potential Applicability ◽  
Bacteria And Fungi ◽  
Positively Charged

AbstractAntimicrobial peptides (AMPs) are a class of short, usually positively charged polypeptides that exist in humans, animals, and plants. Considering the increasing number of drug-resistant pathogens, the antimicrobial activity of AMPs has attracted much attention. AMPs with broad-spectrum antimicrobial activity against many gram-positive bacteria, gram-negative bacteria, and fungi are an important defensive barrier against pathogens for many organisms. With continuing research, many other physiological functions of plant AMPs have been found in addition to their antimicrobial roles, such as regulating plant growth and development and treating many diseases with high efficacy. The potential applicability of plant AMPs in agricultural production, as food additives and disease treatments, has garnered much interest. This review focuses on the types of plant AMPs, their mechanisms of action, the parameters affecting the antimicrobial activities of AMPs, and their potential applications in agricultural production, the food industry, breeding industry, and medical field.

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, Molecular Docking and Antimicrobial Evaluation of Some Benzothiazoles

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Property ◽  
Docking Study ◽  
Gram Negative Bacteria ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Good Antibacterial Activity ◽  
Comparable Activity ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi

Abstract Abstract The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.

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 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).

Environmentally benign one-pot synthesis and antimicrobial activity of 1-methyl-2,6-diarylpiperidin-4-ones

2011 ◽  
Vol 65 (5) ◽  
Author(s):  
Pattusamy Nithya ◽  
Fazlur-Rahman Nawaz Khan ◽  
Selvaraj Roopan ◽  
Uma Shankar ◽  
Jong Jin
Keyword(s):  
Antimicrobial Activity ◽  
Environmentally Benign ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
One Pot ◽  
Gram Negative ◽  
One Pot Synthesis ◽  
Bacteria And Fungi

AbstractAn efficient and environmentally benign one-pot method for the synthesis of 1-methyl-2,6-diarylpiperidin-4-ones using montmorillonite K-10 as a catalyst has been developed. Antimicrobial activity of the compounds has been tested against selected representatives of Gram-positive and Gram-negative bacteria and fungi.

scholarly journals Synthesis, antioxidant and antimicrobial activity of carbohydrazones

2017 ◽  
Vol 82 (5) ◽  
pp. 495-508 ◽  
Author(s):  
Aleksandra Bozic ◽  
Nenad Filipovic ◽  
Irena Novakovic ◽  
Snezana Bjelogrlic ◽  
Jasmina Nikolic ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Dimethyl Sulphoxide ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Antioxidant Compound ◽  
Antioxidant And Antimicrobial Activity ◽  
Bacteria And Fungi

Fourteen mono- and bis-carbohydrazone ligands have been synthesized and characterized. Antioxidant activity of the substances was investigated together with possible (E)/(Z) isomerization, and explained on the most active antioxidant compound 4 in various dimethyl sulphoxide?water mixtures. The addition of water to the system was involved in the formation of hydrated molecules which was confirmed in NMR after the addition of D2O. The ligands were tested in vitro against Gram-positive and Gram-negative bacteria and fungi, and their activity was discussed in relation to the structure of investigated carbohydrazone.

scholarly journals Antimicrobial activity of the rhizomes of Curcuma zedoaria

1970 ◽  
Vol 34 (2) ◽  
pp. 201-203 ◽  
Author(s):  
Mohammad Shahriar
Keyword(s):  
Antimicrobial Activity ◽  
Ethyl Acetate ◽  
Moderate Activity ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Curcuma Zedoaria ◽  
Gram Negative ◽  
Successive Extraction ◽  
Bacteria And Fungi ◽  
Academy Of Sciences

Successive extraction of the dried rhizomes of Curcuma zedoaria Rocs. provided n-hexane, ethyl acetate and methanol extracts. The antimicrobial activity of the different extracts of Curcuma zedoaria was investigated at an initial dose of 500 μg/disc against gram positive, gram negative bacteria and fungi. The methanol extract of the herb showed significant activity against some tested gram negative bacteria. The ethyl acetate extract exhibited moderate activity while the n-hexane showed little activity against some gram negative bacteria.Key words: Curcuma zedoaria; Rhizomes; Antimicrobial activity DOI: 10.3329/jbas.v34i2.6867Journal of Bangladesh Academy of Sciences, Vol. 34, No. 2, 201-203, 2010

scholarly journals Synthesis of certain pyrrole derivatives as antimicro-bial agents

2009 ◽  
Vol 59 (2) ◽  
pp. 145-158 ◽  
Author(s):  
Mosaad Mohamed ◽  
Ramdan El-Domany ◽  
Rania Abd El-Hameed
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Amines ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Pyrrole Derivatives ◽  
Gram Negative ◽  
Primary Aromatic Amines ◽  
Aryl Amines ◽  
Bacteria And Fungi

Synthesis of certain pyrrole derivatives as antimicro-bial agentsIn an effort to establish new pyrroles and pyrrolo[2,3-d] pyrimidines with improved antimicrobial activity we report here the synthesis andin vitromicrobiological evaluation of a series of pyrrole derivatives. A series of new 2-aminopyrrole-3-carbonitriles (1a-d) were synthesized from the reaction of benzoin, primary aromatic amines and malononitrile, from which a number of pyrrole derivatives (2a-dto5a-d) and pyrrolo[2,3-d]pyrimidines (6a-dto10a, d) were synthesized. Thein vitroantimicrobial testing of the synthesized compounds was carried out against Gram-positive, Gram-negative bacteria and fungi. Some of the prepared compounds, [2-amino-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrole-3-carbonitriles (1b), 2-amino-3-carbamoyl-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrroles (2b),N-(3-cyano-1-(2-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3b),N-(3-cyano-1-(3-methylphenyl)-4,5-diphenyl-1H-pyrrol-2-yl)-acetamides (3c), 2-amino-1-(4-methoxyphenyl)-4,5-diphenyl-3-tetrazolo-1H-pyrroles (5d),7-(4-methoxyphenyl)-5,6-diphenyl-7H-pyrrolo [2,3-d]pyrimidin-4(3H)-ones (7d), 7-(3-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-thione (9b) andN-(7-(2-methylphenyl)-5,6-diphenyl-7H-pyrrolo[2,3-d] pyrimidine)-N-aryl amines (10a)] showed potent antimicrobial activity.

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.

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