78295-91-7Relevant academic research and scientific papers
Bacteria-triggered release of antimicrobial agents
Komnatnyy, Vitaly V.,Chiang, Wen-Chi,Tolker-Nielsen, Tim,Givskov, Michael,Nielsen, Thomas E.
supporting information, p. 439 - 441 (2014/01/23)
Medical devices employed in healthcare practice are often susceptible to microbial contamination. Pathogenic bacteria may attach themselves to device surfaces of catheters or implants by formation of chemically complex biofilms, which may be the direct cause of device failure. Extracellular bacterial lipases are particularly abundant at sites of infection. Herein it is shown how active or proactive compounds attached to polymeric surfaces using lipase-sensitive linkages, such as fatty acid esters or anhydrides, may be released in response to infection. Proof-of-concept of the responsive material is demonstrated by the bacteria-triggered release of antibiotics to control bacterial populations and signaling molecules to modulate quorum sensing. The self-regulating system provides the basis for the development of device-relevant polymeric materials, which only release antibiotics in dependency of the titer of bacteria surrounding the medical device. Bacteria-responsive materials: A new approach for the construction of antimicrobial polymeric materials is presented. Optimized solid-phase synthesis protocols provide access to drug hybrid constructs with lipase-labile chemical bonds. Upon cleavage of this labile bond by a cognate bacterial lipase, the release of antimicrobial compounds is triggered (see picture).
Novel antibacterial class: A series of tetracyclic derivatives
Hinman, Mira M.,Rosenberg, Teresa A.,Balli, Darlene,Black-Schaefer, Candace,Chovan, Linda E.,Kalvin, Douglas,Merta, Philip J.,Nilius, Angela M.,Pratt, Steve D.,Soni, Niru B.,Wagenaar, Frank L.,Weitzberg, Moshe,Wagner, Rolf,Beutel, Bruce A.
, p. 4842 - 4856 (2007/10/03)
We describe the synthesis and antibacterial activity of a series of tetracyclic naphthyridones. The members of this series act primarily via inhibition of bacterial translation and belong to the class of novel ribosome inhibitors (NRIs). In this paper we
