Unknown

Dataset Information

0

Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.

ABSTRACT: Therapeutic options for brain infections caused by pathogens with a reduced sensitivity to drugs are limited. Recent reports on the potential use of linezolid in treating brain infections prompted us to design novel compounds around this scaffold. Herein, we describe the design and synthesis of various oxazolidinone antibiotics with the incorporation of silicon. Our findings in preclinical species suggest that silicon incorporation is highly useful in improving brain exposures. Interestingly, three compounds from this series demonstrated up to a 30-fold higher brain/plasma ratio when compared to linezolid thereby indicating their therapeutic potential in brain associated disorders.

SUBMITTER: Seetharamsingh B 

PROVIDER: S-EPMC4645245 | biostudies-other | 2015 Nov

REPOSITORIES: biostudies-other

Json Xml
altmetric image

Publications

Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.

Seetharamsingh B B   Ramesh Remya R   Dange Santoshkumar S SS   Khairnar Pankaj V PV   Singhal Smita S   Upadhyay Dilip D   Veeraraghavan Sridhar S   Viswanadha Srikant S   Vakkalanka Swaroop S   Reddy D Srinivasa DS  

ACS medicinal chemistry letters 20151026 11

Therapeutic options for brain infections caused by pathogens with a reduced sensitivity to drugs are limited. Recent reports on the potential use of linezolid in treating brain infections prompted us to design novel compounds around this scaffold. Herein, we describe the design and synthesis of various oxazolidinone antibiotics with the incorporation of silicon. Our findings in preclinical species suggest that silicon incorporation is highly useful in improving brain exposures. Interestingly, th  ...[more]

Similar Datasets

Unknown Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation.
| S-EPMC4645241 | biostudies-literature
Unknown Oxazolidinone Antibiotics: Chemical, Biological and Analytical Aspects.
| S-EPMC8305375 | biostudies-literature
Other Structural basis for PoxtA-mediated resistance to Phenicol and Oxazolidinone antibiotics 
2022-02-12 | GSE179348 | GEO
Unknown Structure-guided design, synthesis and evaluation of oxazolidinone-based inhibitors of norovirus 3CL protease.
| S-EPMC5737831 | biostudies-literature
Unknown Pyrazole Incorporated New Thiosemicarbazones: Design, Synthesis and Investigation of DPP-4 Inhibitory Effects.
| S-EPMC7662656 | biostudies-literature
Unknown The oxazolidinone antibiotics perturb the ribosomal peptidyl-transferase center and effect tRNA positioning.
| S-EPMC2533191 | biostudies-literature
Unknown Design, synthesis and anticancer activity of some novel thioureido-benzenesulfonamides incorporated biologically active moieties.
| S-EPMC4823908 | biostudies-literature
Unknown Design, synthesis and microbiological evaluation of ampicillin-tetramic acid hybrid antibiotics.
| S-EPMC5116011 | biostudies-literature
Unknown Synthesis of Oxazolidinone and Tosyl Enamines by Tertiary Amine Catalysis.
| S-EPMC3059314 | biostudies-literature
Transcriptomics Identification of a Mammalian Silicon Transporter
2017-04-05 | GSE58404 | GEO