39263-68-8Relevant academic research and scientific papers
1,2,4-TRIAZOLIDINE-3-THIONE DERIVATIVES AND USES THEREOF
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Page/Page column 34; 45; 46, (2018/03/09)
The present invention relates to 1,2,4-triazolidine-3-thione compounds, compositions, and methods for the treatment or prevention of bacterial infections (for example, bacterial infections due to Acinetobacter).
1,2,4-Triazolidine-3-thiones as narrow spectrum antibiotics against multidrug-resistant acinetobacter baumannii
Huggins, William M.,Minrovic, Bradley M.,Corey, Brendan W.,Jacobs, Anna C.,Melander, Roberta J.,Sommer, Roger D.,Zurawski, Daniel V.,Melander, Christian
supporting information, p. 27 - 31 (2017/12/12)
With only two new classes of antibiotics developed in the last 40 years, novel antibiotics are desperately needed to combat the growing problem of multidrug-resistant and extensively drug resistant bacteria, particularly Gram-negative bacteria. Described in this letter is the synthesis and antibiotic activity of 1,2,4-triazolidine-3-thiones as narrow spectrum antibiotics. Optimization of the 1,2,4-triazolidine-3-thione scaffold identified a small molecule with potent antibiotic activity against multiple strains of multidrug-resistant and extensively drug-resistant Acinetobacter baumannii. This small molecule also shows single dose, in vivo activity in a Galleria mellonella infection model with A. baumannii and represents a promising start in the development of a class of drugs that can target this bacterial pathogen.
