2209871-83-8
Chemical Structure
ETX0282
- CAS No.: 2209871-83-8
- Formula:C13H18FN3O5
- Molecular Weight:315.30
IUPAC Name: isopropyl (R)-2-(((1R,2S,5R)-2-carbamoyl-4-methyl-7-oxo-1,6-diazabicyclo[3.2.1]oct-3-en-6-yl)oxy)-2-fluoroacetate
InChIKey: OMNVFPBGXYKTDB-GUBZILKMSA-N
SMILES: O=C(OC(C)C)[C@H](ON1[C@]2([H])C(C)=C[C@@H](C(N)=O)[N@@](C2)C1=O)F
Biological Activity: ETX0282 is an orally active prodrug, with its active form being ETX1317. ETX0282 and ETX1317 are β-lactamase inhibitors of the dioxolane-dibenzo-p-heptane (DBO) type. ETX0282 exhibits high stability during intestinal absorption and can be efficiently converted into ETX1317 in the liver. ETX0282 alone has no bactericidal activity, but in a mouse model of neutropenic thigh infection, it can significantly reduce bacterial load when used in combination with Cefpodoxime Proxetil (HY-N7101). ETX0282 can be used for the study of infections caused by drug-resistant Gram-negative bacteria[1][2].
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ETX0282 | ETX0282 is an orally active prodrug, with its active form being ETX1317. ETX0282 and ETX1317 are β-lactamase inhibitors of the dioxolane-dibenzo-p-heptane (DBO) type. ETX0282 exhibits high stability during intestinal absorption and can be efficiently converted into ETX1317 in the liver. ETX0282 alone has no bactericidal activity, but in a mouse model of neutropenic thigh infection, it can significantly reduce bacterial load when used in combination with Cefpodoxime Proxetil (HY-N7101). ETX0282 can be used for the study of infections caused by drug-resistant Gram-negative bacteria. | |||||||||||||||||||||
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References
- [1]. Durand-Réville TF, et al. Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases. J Med Chem. 2020 Nov 12;63(21):12511-12525. [Content Brief]
- [2]. O'Donnell J, et al. Pharmacokinetic/Pharmacodynamic Determination and Preclinical Pharmacokinetics of the β-Lactamase Inhibitor ETX1317 and Its Orally Available Prodrug ETX0282. ACS Infect Dis. 2020 Jun 12;6(6):1378-1388. [Content Brief]
