Till sidans topp

Sidansvarig: Webbredaktion
Sidan uppdaterades: 2012-09-11 15:12

Tipsa en vän
Utskriftsversion

Development and evaluatio… - Göteborgs universitet Till startsida
Webbkarta
Till innehåll Läs mer om hur kakor används på gu.se

Development and evaluation of cationic amphiphilic antimicrobial 2,5-diketopiperazines

Artikel i vetenskaplig tidskrift
Författare C. Labriere
Nahid Kondori
J. S. Caous
M. Boomgaren
K. Sandholm
K. N. Ekdahl
J. H. Hansen
J. Svenson
Publicerad i Journal of Peptide Science
Volym 24
Nummer/häfte 7
ISSN 1075-2617
Publiceringsår 2018
Publicerad vid Institutionen för biomedicin, avdelningen för infektionssjukdomar
Språk en
Länkar dx.doi.org/10.1002/psc.3090
Ämnesord 2,5-diketopiperazine, antifungal agents, antimicrobial, Candida krusei, MRSA, structure-activity, blood-stream infections, candida-albicans, antibacterial peptides, staphylococcus-aureus, methicillin-resistant, antifungal activity, fungal-infections, oral candidiasis, defense, lactoferricin, Biochemistry & Molecular Biology, Chemistry
Ämneskategorier Biokemi och molekylärbiologi

Sammanfattning

Both pathogenic bacteria and fungi are developing resistance to common antimicrobial treatment at an alarming rate. To counteract this development, it is of essence to develop new classes of antimicrobial agents. One such class is antimicrobial peptides, most of which are derived from the innate immune system. In this study, a series of novel 2,5-diketopiperazines were designed, synthesized, and evaluated for their antimicrobial abilities. The compounds were designed to probe the pharmacophore dictated for short linear mimics of antimicrobial cationic peptides, and as such, the compounds contain a range of cationic and hydrophobic functionalities. Several of the prepared compounds displayed high antimicrobial activities toward bacteria and also against human pathogenic fungi. Of particular interest was the high activity toward fungal strains with an inherent increased resistance toward conventional antifungal agents. The most effective compounds displayed inhibition of Candida glabrata and Candida krusei growth at concentrations between 4 and 8 mu g/mL, which is comparable to commercial antifungal agents in use. Structure activity relationship studies revealed a similar dependence on cationic charge and the volume of the hydrophobic bulk as for linear cationic antimicrobial peptides. Finally, the hemolytic activity of selected compounds was evaluated, which revealed a potential to produce active compounds with attenuation of unwanted hemolysis. The findings highlight the potential of cyclic cationic amphiphilic peptidomimetics as a class of promising compounds for the treatment of infections caused by microorganisms with an increased resistance to conventional antimicrobial agents.

Sidansvarig: Webbredaktion|Sidan uppdaterades: 2012-09-11
Dela:

På Göteborgs universitet använder vi kakor (cookies) för att webbplatsen ska fungera på ett bra sätt för dig. Genom att surfa vidare godkänner du att vi använder kakor.  Vad är kakor?