1430321-59-7Relevant articles and documents
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure
Seetharamsingh,Ramesh, Remya,Dange, Santoshkumar S.,Khairnar, Pankaj V.,Singhal, Smita,Upadhyay, Dilip,Veeraraghavan, Sridhar,Viswanadha, Srikant,Vakkalanka, Swaroop,Reddy, D. Srinivasa
, p. 1105 - 1110 (2015/11/24)
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.
SILA ANALOGS OF OXAZOLIDINONE DERIVATIVES AND SYNTHESIS THEREOF
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, (2013/04/25)
The invention discloses silaanalogs of oxazolidinone compounds, to pharmaceutical compositions and to the synthesis of the oxazolidinone derivatives of formula I. The invention further relates to methods of treating a subject suffering with gram positive pathogens including those resistant to methicillin and vancomycin using the compound(s) or modulation of coagulation properties of blood-clotting cascade or compositions of the oxazolidinone derivatives of the invention.