Name: (S)-2-Amino-2-(4-fluorophenyl)ethanol《Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity》 was published in 2018. The authors were Skepper, Colin K.;Moreau, Robert J.;Appleton, Brent A.;Benton, Bret M.;Drumm, Joseph E.;Feng, Brian Y.;Geng, Mei;Hu, Cheng;Li, Cindy;Lingel, Andreas;Lu, Yipin;Mamo, Mulugeta;Mergo, Wosenu;Mostafavi, Mina;Rath, Christopher M.;Steffek, Micah;Takeoka, Kenneth T.;Uehara, Kyoko;Wang, Lisha;Wei, Jun-Rong;Xie, Lili;Xu, Wenjian;Zhang, Qiong;de Vicente, Javier, and the article was included in《Journal of Medicinal Chemistry》. The author mentioned the following in the article:
In the preceding manuscript the authors described a successful fragment-based lead discovery (FBLD) strategy for discovery of bacterial phosphopantetheine adenylyltransferase inhibitors (PPAT, CoaD). Following several rounds of optimization two promising lead compounds were identified: triazolopyrimidinone (I) and 4-azabenzimidazole (II). Here the authors disclose the efforts to further optimize these two leads for on-target potency and Gram-neg. cellular activity. Enabled by a robust x-ray crystallog. system, the authors’ structure-based inhibitor design approach delivered compounds with biochem. potencies 4-5 orders of magnitude greater than their resp. fragment starting points. Addnl. optimization was guided by observations on bacterial permeability and physicochem. properties, which ultimately led to the identification of PPAT inhibitors with cellular activity against wild-type E. coli. The experimental procedure involved many compounds, such as (S)-2-Amino-2-(4-fluorophenyl)ethanol (cas: 224434-01-9) .
(S) – 2-amino-2 – (4-fluorophenyl) ethanol (cas: 224434-01-9) has the characteristics of alcohol. In general, the hydroxyl group makes alcohols polar. Those groups can form hydrogen bonds to one another and to most other compounds. Name: (S)-2-Amino-2-(4-fluorophenyl)ethanol
Reference:
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