Publications by authors named "Maria T Stranieri"
Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.
Christopher S Burgey Kyle A Robinson Terry A Lyle Philippe G Nantermet Harold G Selnick Maria T Stranieri
Bioorg Med Chem Lett
April 2003
In this manuscript we demonstrate that a modification principally directed toward the improvement of the aqueous solubility (i.e., introduction a P3 pyridine N-oxide) of the previous lead compound afforded a new series of potent orally bioavailable P1 N-benzylamide thrombin inhibitors.
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- Recent research on thrombin inhibitors is concentrating on finding compounds that are effective when taken orally and have good pharmacokinetics.
- A new approach was used to improve a specific compound framework (3-(2-phenethylamino)-6-methylpyrazinone acetamide) by modifying its main components.
- The result was the discovery of several strong thrombin inhibitors that are not only potent but also have high oral bioavailability and extended plasma half-lives.