AI Article Synopsis
- 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.
Article Abstract
Recent efforts in the field of thrombin inhibitor research have focused on the identification of compounds with good oral bioavailability and pharmacokinetics. In this manuscript we describe a metabolism-based approach to the optimization of the 3-(2-phenethylamino)-6-methylpyrazinone acetamide template (e.g., 1) which resulted in the modification of each of the three principal components (i.e., P1, P2, P3) comprising this series. As a result of these studies, several potent thrombin inhibitors (e.g., 20, 24, 25) were identified which exhibit high levels of oral bioavailability and long plasma half-lives.
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| http://dx.doi.org/10.1021/jm020311f | DOI Listing |
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