Synthesis and evaluation of membrane permeabilizing properties of cationic amphiphiles derived from the disaccharide trehalose

2016 ◽  
Vol 14 (11) ◽  
pp. 3012-3015 ◽  
Author(s):  
P. Shaul ◽  
R. I. Benhamou ◽  
I. M. Herzog ◽  
S. Louzoun Zada ◽  
Y. Ebenstein ◽  
...  

Cationic amphiphiles derived from trehalose have been synthesized; trehalose analogues substituted withn-pentyl orn-hexyl ethers exhibited membrane disrupting activities against clinically important Gram positive and Gram negative bacteria and fungi.

2019 ◽  
Vol 43 (9-10) ◽  
pp. 307-312
Author(s):  
Amira A El-Sayed ◽  
Saad R Atta-Allah ◽  
Magdy M Hemdan

Convenient syntheses of quinazoline, benzothiazole, thiadiazole, imidazole, and thiourea derivatives starting from 3-(thiophen-2-yl)prop-2-enoyl isothiocyanate are described. The structures of the synthesized compounds are confirmed from their microanalytical and spectral data. Some of the products are examined for their antibacterial activity against Gram-positive and Gram-negative bacteria and fungi.


2011 ◽  
Vol 65 (5) ◽  
Author(s):  
Pattusamy Nithya ◽  
Fazlur-Rahman Nawaz Khan ◽  
Selvaraj Roopan ◽  
Uma Shankar ◽  
Jong Jin

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.


2017 ◽  
Vol 82 (5) ◽  
pp. 495-508 ◽  
Author(s):  
Aleksandra Bozic ◽  
Nenad Filipovic ◽  
Irena Novakovic ◽  
Snezana Bjelogrlic ◽  
Jasmina Nikolic ◽  
...  

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.


2009 ◽  
Vol 59 (2) ◽  
pp. 145-158 ◽  
Author(s):  
Mosaad Mohamed ◽  
Ramdan El-Domany ◽  
Rania Abd El-Hameed

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.


MedChemComm ◽  
2016 ◽  
Vol 7 (1) ◽  
pp. 86-102 ◽  
Author(s):  
Kfir B. Steinbuch ◽  
Micha Fridman

A diverse repertoire of mechanisms has evolved to confer resistance to bacterial membrane disrupting antimicrobial cationic amphiphiles.


Author(s):  
Runa S. Boeddinghaus ◽  
Sven Marhan ◽  
Aurelia Gebala ◽  
Heike Haslwimmer ◽  
Selma Vieira ◽  
...  

AbstractTo improve our understanding of early microbial colonization of pristine minerals and their group-specific C utilization, we exposed minerals (illite/goethite/quartz) amended with artificial root exudates (ARE, glucose, and citric acid) in grassland soils for a period of 24 weeks. FTIR spectra indicated that mineral-associated ARE were used within the first 2 weeks of exposure and were replaced by other carbohydrates derived from living or dead cells as well as soil-borne C sources transported into the mineralosphere after heavy rain events. Fungi and Gram-positive bacteria incorporated ARE-derived C more rapidly than Gram-negative bacteria. Gram-negative bacteria presumably profited indirectly from the ARE by cross-feeding on mineral-associated necromass of fungi and Gram-positive bacteria. The Gram-negative bacterial phyla Verrucomicrobia, Planctomycetes, Gemmatimonadetes, Armatimonadetes, and Chloroflexi showed a positive correlation with Gram-negative PLFA abundances. After 24 weeks of exposure in the grassland soils, abundances of soil microorganisms in the mineralosphere reached only 3.1% of the population density in soil. In conclusion, both bacteria and fungi slowly colonize new surfaces such as pristine minerals, but quickly assimilate artificial root exudates, creating an active microbial community in the mineralosphere.


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