2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors
Copyright policy )2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors
TNF-α converting enzyme (TACE) inhibitors are promising agents to treat inflammatory disorders and cancer. We have investigated novel tartrate diamide TACE inhibitors where the tartrate core binds to zinc in a unique tridentate fashion. Incorporating (R)-2-(2-N-alkylaminothiazol-4-yl)pyrrolidines into the left hand side amide of the tartrate scaffold led to the discovery of potent and selective TACE inhibitors, some of which exhibited good rat oral bioavailability.
- Merck & Co. United States
Pyrrolidines, Molecular Structure, Biological Availability, ADAM17 Protein, Amides, Rats, Enzyme Activation, ADAM Proteins, Animals, Enzyme Inhibitors, Tartrates
Pyrrolidines, Molecular Structure, Biological Availability, ADAM17 Protein, Amides, Rats, Enzyme Activation, ADAM Proteins, Animals, Enzyme Inhibitors, Tartrates
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