Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.
Tomczuk B,
Lu T,
Soll RM,
Fedde C,
Wang A,
Murphy L,
Crysler C,
Dasgupta M,
Eisennagel S,
Spurlino J,
Bone R.
3-Dimensional Pharmaceuticals, Inc., 665 Stockton Drive, Exton, PA 19341, USA. bruce.tomczuk@3dp.com
Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive. We report here a novel series non-peptidic phenyl-based, highly potent, highly selective and orally bioavailable thrombin inhibitors using oxyguanidines as guanidine-mimetics.
PMID: 12668020 [PubMed - indexed for MEDLINE]