4133-72-6Relevant academic research and scientific papers
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens
Wu, Yongqi,Wang, Bin,Lu, Haijia,Zhao, Hongyi,Yang, Beibei,Li, Li,Lu, Yu,Zhang, Dongfeng,Sun, Ning,Huang, Haihong
, p. 3234 - 3248 (2021/04/06)
A series of conformationally constrained novel benzo[1,3]oxazinyloxazolidinones were designed, synthesized, and evaluated on their activities against Mycobacterium tuberculosis, Gram-positive bacteria, and Gram-negative bacteria. The studies identified a new compound 20aa that displayed good to excellent antibacterial and antitubercular profiles against drug-resistant TB strains (MIC = 0.48-0.82 μg/mL), MRSA (MIC = 0.25-0.5 μg/mL), MRSE (MIC = 1 μg/mL), VISA (MIC = 0.25 μg/mL), and VRE (MIC = 0.25 μg/mL) and some linezolid-resistant strains (MIC 1-2 μg/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-∞ = 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.
Benzo[1, 3]oxazin-oxazolidinone compounds, and preparation method and application thereof
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, (2021/08/07)
The invention discloses benzo[1, 3]oxazin-oxazolidinone compounds, and a preparation method and application thereof, and belongs to the technical field of medicines. The invention specifically relates to application in preparation of drugs for treating an
APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS AND USES THEREOF
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, (2019/04/09)
Described herein are ASK1 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of blood disease, autoimmune disorders, pulmonary disorders, hypertension, inflammatory diseases, fibrotic diseases, diabetes, diabetic nephropathy, renal diseases, respiratory diseases, cardiovascular diseases, acute lung injuries, acute or chronic liver diseases, and neurodegenerative diseases.
Big catkin willow acids compounds and medical use
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, (2019/05/28)
The invention discloses a AMPK agonist activity with salicylic acid compound and its preparation method and medical use, it is the structural formula of the formula (I) compound of formula, its pharmaceutically acceptable salt or prodrug or solvate. The structure of the invention of formula (I) compound of formula activated AMPK, therefore can be used for preparing the prevention or treatment of AMPK mediated diseases.
ASK1 INHIBITING AGENTS
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, (2018/09/08)
Provided are compounds of Formulas (I'), (I), (II') and (II), or pharmaceutically acceptable salts thereof, and methods for their use and production.
METHOD FOR PRODUCING PRECURSORS FOR L-3,4-DIHYDROXY-6- [18F] FLUOROPHENYL ALAINE AND 2- [18F] FLUORO-L-TYROSINE AND THE ALPHA-METHYLATED DERIVATIVES THEREOF, PRECURSOR, AND METHOD FOR PRODUCING L-3, 4DIHYDROXY-6- [18F] FLUOROPHENYLALANINE AND 2- [18F] FLU
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Page/Page column 1; 4, (2010/11/03)
Disclosed is a method for producing precursors for L-3,4-dihydroxy-6-[18F]fluorophenylalanine and 2-[18F]fluoro-L-tyrosine and the α-methylated derivatives thereof, the precursor, and to a method for producing L-3,4-dihydroxy-6-[sup
