Wu, Yongqi published the artcileIdentification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens, SDS of cas: 1219707-39-7, the publication is Journal of Medicinal Chemistry (2021), 64(6), 3234-3248, database is CAplus and MEDLINE.
A series of conformationally constrained novel benzo[1,3]oxazinyloxazolidinones were designed, synthesized, and evaluated on their activities against Mycobacterium tuberculosis, Gram-pos. bacteria, and Gram-neg. bacteria. The studies identified a new compound 20aa that displayed good to excellent antibacterial and antitubercular profiles against drug-resistant TB strains (MIC = 0.48-0.82μg/mL), MRSA (MIC = 0.25-0.5μg/mL), MRSE (MIC = 1μg/mL), VISA (MIC = 0.25μg/mL), and VRE (MIC = 0.25μg/mL) and some linezolid-resistant strains (MIC 1-2μg/mL). Compound 20aa was demonstrated as a promising candidate through ADME/T evaluation including microsomal stability, cytotoxicity, and inhibition of hERG and monoamine oxidase. Notably, 20aa showed excellent mouse PK profile with high plasma exposure (AUC0-â?/sub> = 78 669 h·ng/mL), high peak plasma concentration (Cmax = 10 253 ng/mL), appropriate half-life of 3.76 h, and superior oral bioavailability (128%). The present study not only successfully provides a novel benzo[1,3]oxazinyloxazolidinone scaffold with superior druggability but also lays a good foundation for new antibacterial drug development.
Journal of Medicinal Chemistry published new progress about 1219707-39-7. 1219707-39-7 belongs to oxazolidine, auxiliary class Other Aliphatic Heterocyclic,Oxazolidine,Chiral,Fluoride,Benzene,Amide,Alcohol,Anti-infection, name is (R)-3-(3-Fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one, and the molecular formula is C8H14O4, SDS of cas: 1219707-39-7.
Referemce:
https://en.wikipedia.org/wiki/Oxazolidine,
Oxazolidine | C3H7NO – PubChem