Inspiration from Old Dyes: Tris(stilbene) Compounds as Potent Gram‐Positive Antibacterial Agents. Issue 52 (18th November 2013)

• Record Type: Journal Article
• Authors: Boulos, Ramiz A.; Man, Nikki Y. T.; Lengkeek, Nigel A.; Hammer, Katherine A.; Foster, Niki F.; Stemberger, Natalie A.; Skelton, Brian W.; Wong, Pan Yu; Martinac, Boris; Riley, Thomas V.; McKinley, Allan J.; Stewart, Scott G.
• Is Part Of: Chemistry. Volume 19:Issue 52(2013)
• Page Start: 17980
• Page End: 17988
• Publication Date: 2013-11-18
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.201303119
• Languages: English
• ISSNs: 0947-6539

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>Herein we describe the preparation and structure‐activity relationship studies on range of stilbene based compounds and their antibacterial activity. Two related compounds, each bearing carboxylic acid moieties, exhibit good activity against several bacterial strains, including methicillin‐resistant <italic>Staphylococcus aureus</italic> MRSA (ATCC 33592 and NCTC 10442). Compound <bold>10</bold> was most active against <italic>Moraxella catarrhalis</italic> with minimum inhibitory concentrations (MICs) of 0.12–0.25 μg mL⁻¹ and against <italic>Staphylococcus spp.</italic> with MICs ranging from 2–4 μg mL⁻¹. The derivative <bold>17</bold> showed increased activity with MICs of 0.06–0.25 μg mL⁻¹ against <italic>M. catarrhalis</italic> and 0.12–1 against <italic>Staphylococcus spp</italic>. This level of activity is similar to that reported for <italic>S. aureus</italic> for antibiotics, such as vancomycin, with MICs of ≤2.0 μg mL⁻¹ and clindamycin with MICs of ≤0.5 μg mL⁻¹. As an indicator of toxicity, <bold>17</bold> was tested for its ability to lyse sheep erythrocytes, and showed low haemolytic activity. Such results highlight the value of tris(stilbene) compounds as antibacterial agents providing suitable properties for further development.</p> </abstract>