01792nas a2200313   4500008004100000022001400041245012100055210006900176260007100245300001400316490000600330520070200336653001801038653001901056653001401075653001801089653001801107100002301125700001801148700002801166700002501194700001901219700002001238700002701258700002401285700002401309700002101333856012401354       2015                        eng d  a1948-587500aDesign, synthesis, and identification of silicon incorporated oxazolidinone antibiotics with improved brain exposure0 aDesign synthesis and identification of silicon incorporated oxaz  a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcNOV  a1105-11100 v63 a<p>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.</p>10aAntibacterial10abrain exposure10alinezolid10aoxazolidinone10asila analogue1 aSeetharamsingh, B.1 aRamesh, Remya1 aDange, Santoshkumar, S.1 aKhairnar, Pankaj, V.1 aSinghal, Smita1 aUpadhyay, Dilip1 aVeeraraghavan, Sridhar1 aViswanadha, Srikant1 aVakkalanka, Swaroop1 aReddy, Srinivasa  uhttps://library.ncl.res.in/content/design-synthesis-and-identification-silicon-incorporated-oxazolidinone-antibiotics-0