<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Seetharamsingh, B.</style></author><author><style face="normal" font="default" size="100%">Ramesh, Remya</style></author><author><style face="normal" font="default" size="100%">Dange, Santoshkumar S.</style></author><author><style face="normal" font="default" size="100%">Khairnar, Pankaj V.</style></author><author><style face="normal" font="default" size="100%">Singhal, Smita</style></author><author><style face="normal" font="default" size="100%">Upadhyay, Dilip</style></author><author><style face="normal" font="default" size="100%">Veeraraghavan, Sridhar</style></author><author><style face="normal" font="default" size="100%">Viswanadha, Srikant</style></author><author><style face="normal" font="default" size="100%">Vakkalanka, Swaroop</style></author><author><style face="normal" font="default" size="100%">Reddy, D. Srinivasa</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Design, synthesis, and identification of silicon incorporated oxazolidinone antibiotics with improved brain exposure</style></title><secondary-title><style face="normal" font="default" size="100%">ACS Medicinal Chemistry Letters</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">Antibacterial</style></keyword><keyword><style  face="normal" font="default" size="100%">brain exposure</style></keyword><keyword><style  face="normal" font="default" size="100%">linezolid</style></keyword><keyword><style  face="normal" font="default" size="100%">oxazolidinone</style></keyword><keyword><style  face="normal" font="default" size="100%">sila analogue</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">NOV</style></date></pub-dates></dates><number><style face="normal" font="default" size="100%">11</style></number><publisher><style face="normal" font="default" size="100%">AMER CHEMICAL SOC</style></publisher><pub-location><style face="normal" font="default" size="100%">1155 16TH ST, NW, WASHINGTON, DC 20036 USA</style></pub-location><volume><style face="normal" font="default" size="100%">6</style></volume><pages><style face="normal" font="default" size="100%">1105-1110</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;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.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">11</style></issue><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">3.355</style></custom4></record><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Ramesh, Remya</style></author><author><style face="normal" font="default" size="100%">Shingare, Rahul D.</style></author><author><style face="normal" font="default" size="100%">Kumar, Vinod</style></author><author><style face="normal" font="default" size="100%">Anand, Amitesh</style></author><author><style face="normal" font="default" size="100%">Swetha, B.</style></author><author><style face="normal" font="default" size="100%">Veeraraghavan, Sridhar</style></author><author><style face="normal" font="default" size="100%">Viswanadha, Srikant</style></author><author><style face="normal" font="default" size="100%">Ummanni, Ramesh</style></author><author><style face="normal" font="default" size="100%">Gokhale, Rajesh S.</style></author><author><style face="normal" font="default" size="100%">Reddy, D. Srinivasa</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Repurposing of a drug scaffold: identification of novel sila analogues of rimonabant as potent antitubercular agents</style></title><secondary-title><style face="normal" font="default" size="100%">European Journal of Medicinal Chemistry</style></secondary-title></titles><dates><year><style  face="normal" font="default" size="100%">2016</style></year><pub-dates><date><style  face="normal" font="default" size="100%">OCT</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">122</style></volume><pages><style face="normal" font="default" size="100%">723-730</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p&gt;The structural similarity between an MmpL3 inhibitor BM212, and a cannabinoid receptor modulator rimonabant, prompted us to investigate the anti-tubercular activity of rimonabant and its analogues. Further optimization, particularly through incorporation of silicon into the scaffold, resulted in new compounds with significant improvement in anti-tubercular activity against Mycobacterium tuberculosis (H37Rv). The sila analogue 18a was found to be the most potent antimycobacterial compound (MIC, 31 ng/mL) from this series with an excellent selectivity index. (C) 2016 Elsevier Masson SAS. All rights reserved.&lt;/p&gt;</style></abstract><custom3><style face="normal" font="default" size="100%">&lt;p&gt;Foreign&lt;/p&gt;</style></custom3><custom4><style face="normal" font="default" size="100%">3.902</style></custom4></record></records></xml>