Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens was written by Wu, Yongqi;Wang, Bin;Lu, Haijia;Zhao, Hongyi;Yang, Beibei;Li, Li;Lu, Yu;Zhang, Dongfeng;Sun, Ning;Huang, Haihong. And the article was included in Journal of Medicinal Chemistry in 2021.Related Products of 4133-72-6 This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, Methyl 5-bromo-4-fluoro-2-hydroxybenzoate (cas: 4133-72-6Related Products of 4133-72-6).
Methyl 5-bromo-4-fluoro-2-hydroxybenzoate (cas: 4133-72-6) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Related Products of 4133-72-6
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary