AI Article Synopsis
- The text discusses the development of new classes of oral medications that inhibit both factor Xa (fXa) and thrombin, which are important for blood clotting.
- The approach involved making slight changes to a specific sulfonamide group in an existing fXa inhibitor to enhance its effectiveness.
- Structural studies were used to explain how these modifications impact the drug's activity.
Article Abstract
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhibitor (E)-2-(5-chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide and these observed activity changes have been rationalised using structural studies.
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| http://dx.doi.org/10.1016/j.bmcl.2007.03.080 | DOI Listing |
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