199181-50-5Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel non-peptide boronic acid derivatives as proteasome inhibitors
Zhang, Jiankang,Shen, Luqing,Wang, Jincheng,Luo, Peihua,Hu, Yongzhou
, p. 38 - 45 (2014/01/17)
A series of novel non-peptide boronic acid derivatives were designed and synthesized via rational drug design principles. All target compounds were screened for the proteasome inhibitory activities in vitro. Selected compounds (6a and 7j) were evaluated f
Discovery and initial development of a novel class of antibacterials: Inhibitors of Staphylococcus aureus transcription/translation
Larsen, Scott D.,Hester, Matthew R.,Craig Ruble,Kamilar, Gregg M.,Romero, Donna L.,Wakefield, Brian,Melchior, Earline P.,Sweeney, Michael T.,Marotti, Keith R.
, p. 6173 - 6177 (2007/10/03)
The novel bacterial transcription/translation (TT) inhibitor 1 was identified through a combination of high throughput screening and exploratory medicinal chemistry. Initial optimization of the anthranilic acid moiety and sulfonamide amine diversity was accomplished via 1- and two-dimensional solution phase libraries, resulting in an improvement in the MIC of the lead from 64 to 8 μg/mL (compound 4l). Subsequent modification of the central aromatic ring and further refinement of the sulfonamide amines required the development of a solid phase route on Wang resin. The resulting libraries generated a number of potent antibacterials with MICs of ≤1 μg/mL (e.g., 10b, 12, and 13). During the course of this work, it became apparent that the antibacterial activity of the series is not fully correlated with TT inhibition, suggesting that at least one additional mechanism of action is operative.
