1235489-53-8Relevant academic research and scientific papers
Synthesis of Benzothiophene-Containing 10- and 11-Membered Cyclic Phostones
Matralis, Alexios N.,Tsantrizos, Youla S.
, p. 3728 - 3736 (2016/08/16)
Phosphinate and phosphonate derivatives can serve as useful transition-state analogues of proteases, as substrate mimics of DNA/RNA-processing enzymes, and as inhibitors of enzymes catalyzing the biosynthesis of isoprenoids. Synthetic methodologies for the preparation of medium-sized ring phosphonate-containing compounds (also known as phostones are currently limited to a few examples. A synthetic protocol was developed that is amenable to the parallel synthesis of structurally diverse phostones containing a benzo[b]thiophene core, which enables the profiling of such novel compounds in biological screens of potential therapeutic targets.
Combinatorial approach toward synthesis of small molecule libraries as bacterial transglycosylase inhibitors
Shih, Hao-Wei,Chen, Kuo-Ting,Chen, Shao-Kang,Huang, Chia-Ying,Cheng, Ting-Jen R,Ma, Che,Wong, Chi-Huey,Cheng, Wei-Chieh
scheme or table, p. 2586 - 2593 (2010/08/07)
The development of iminocyclitol-based small molecule libraries against a bacterial TGase is described. An iminocyclitol was conjugated with a pyrophosphate mimic using either a 1,3-dipolar cycloaddition or reductive amination reaction, which was then condensed with a variety of lipophilic carboxylic acids in an amide bond coupling to generate a desired molecular library. With assistance of microtiter plate-based combinatorial chemistry and in situ screening, a potential inhibitor, the first potent iminocyclitol-based inhibitor against bacterial TGases was efficiently developed. The Royal Society of Chemistry 2010.
