- A new class of fluorescent boronic acids that have extraordinarily high affinities for diols in aqueous solution at physiological pH
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The boronic acid group is an important recognition moiety for sensor design. Herein, we report a series of isoquinolinylboronic acids that have extraordinarily high affinities for diol-containing compounds at physiological pH. In addition, 5- and 8-isoquinolinylboronic acids also showed fairly high binding affinities towards D-glucose (Ka=42 and 46M-1, respectively). For the first time, weak but encouraging binding of cis-cyclohexanediol was found for these boronic acids. Such binding was coupled with significant fluorescence changes. Furthermore, 4- and 6- isoquinolinylboronic acids also showed the ability to complex methyl α-D-glucopyranose (Ka=3 and 2M-1, respectively). Be the first! The diol-binding behavior of a series of isoquinolinylboronic acids was investigated by monitoring the changes of their fluorescence intensity (see figure for an example, 6-IQBA=6-isoquinolinylboronic acid). For the first time, a boronic acid derivative that binds cis-cyclohexanediol was identified. Copyright
- Cheng, Yunfeng,Ni, Nanting,Yang, Wenqian,Wang, Binghe
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- HETEROCYCLIC INHIBITORS OF PCSK9
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This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I): (I) wherein A, D and Q are described herein.
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(2018/10/24)
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