Protonation activates anion binding and alters binding selectivity in new inherently fluorescent 2,6-bis(2-anilinoethynyl)pyridine bisureas

2009 ◽  
pp. 2520 ◽  
Author(s):  
Calden N. Carroll ◽  
Orion B. Berryman ◽  
Charles A. Johnson ◽  
Lev N. Zakharov ◽  
Michael M. Haley ◽  
...  
2003 ◽  
Vol 5 (26) ◽  
pp. 4971-4974 ◽  
Author(s):  
Gamolwan Tumcharern ◽  
Thawatchai Tuntulani ◽  
Simon J. Coles ◽  
Michael B. Hursthouse ◽  
Jeremy D. Kilburn

ChemInform ◽  
2009 ◽  
Vol 40 (35) ◽  
Author(s):  
Calden N. Carroll ◽  
Orion B. Berryman ◽  
Charles A. II Johnson ◽  
Lev N. Zakharov ◽  
Michael M. Haley ◽  
...  

1997 ◽  
Vol 77 (03) ◽  
pp. 498-503 ◽  
Author(s):  
D Prasa ◽  
L Svendsen ◽  
J Stürzebecher

SummaryIn a thrombin generation test with continuous registration of thrombin activity in plasma we studied the ability of a variety of thrombin inhibitors of different type and mechanism of action to influence the activity of thrombin after activation of the coagulation system. Depending on the inhibitor, the peak of thrombin activity is delayed and/or reduced.By blocking the active site of generated thrombin inhibitors cause a concentration dependent reduction of the thrombin peak and inhibit feed-back reactions of thrombin resulting in a delay of thrombin generation. Highly potent synthetic active-site directed inhibitors (Ki ≤ 20 nM) reduce the thrombin activity formed in plasma after extrinsic or intrinsic activation with the same efficiency (IC50 0.1 - 0.6 μM) as hirudin. The delay and reduction of thrombin generation by inhibitors of the anion-binding exosite 1 of thrombin is only attributed to an inhibition of feed-back reactions of thrombin. For a 50% reduction of thrombin activity in plasma by this type of inhibitors relatively high concentrations were determined.


2019 ◽  
Author(s):  
Riley J. Petersen ◽  
Brett J. Rozeboom ◽  
Shalisa Oburn ◽  
Nolan Blythe ◽  
Tanner Rathje ◽  
...  

<div>We report the synthesis of a novel macrocyclic host molecule that forms in a single step from commercially available starting materials. The core of the macrocycle backbone possesses two quinone rings and, thus, is redox-active. Host-guest binding involving the clip-shaped cavity indicates selective binding of pyridine <i>N</i>-oxides based of the electron density of and steric bulk of the anionic oxygen.</div>


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