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Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics

✍ 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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Amidinohydrazones as guanidine bioisoste
✍ Richard M. Soll; Tianobao Lu; Bruce Tomczuk; Carl R. Illig; Cynthia Fedde; Steph πŸ“‚ Article πŸ“… 2000 πŸ› Elsevier Science 🌐 English βš– 228 KB

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