Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics
β Scribed by Tang, Haifeng; Walsh, Shawn P.; Yan, Yan; de Jesus, Reynalda K.; Shahripour, Aurash; Teumelsan, Nardos; Zhu, Yuping; Ha, Sookhee; Owens, Karen A.; Thomas-Fowlkes, Brande S.; Felix, John P.; Liu, Jessica; Kohler, Martin; Priest, Birgit T.; Bailey, Timothy; Brochu, Richard; Alonso-Galicia, Magdalena; Kaczorowski, Gregory J.; Roy, Sophie; Yang, Lihu; Mills, Sander G.; Garcia, Maria L.; Pasternak, Alexander
- Book ID
- 120426696
- Publisher
- American Chemical Society
- Year
- 2012
- Tongue
- English
- Weight
- 624 KB
- Volume
- 3
- Category
- Article
- ISSN
- 1948-5875
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We describe a new class of potent, non-amide-based small molecule thrombin inhibitors in which an amidinohydrazone is used as a guanidine bioisostere on a non-peptide scaffold. Compound 4 exhibits nM inhibition of thrombin, is selective for thrombin, and shows 60 and 23% bioavailability in rabbits a