@article { ISI:000364803200005,
	title = {Design, synthesis, and identification of silicon incorporated oxazolidinone antibiotics with improved brain exposure},
	journal = {ACS Medicinal Chemistry Letters},
	volume = {6},
	number = {11},
	year = {2015},
	month = {NOV},
	pages = {1105-1110},
	publisher = {AMER CHEMICAL SOC},
	address = {1155 16TH ST, NW, WASHINGTON, DC 20036 USA},
	abstract = {<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>},
	keywords = {Antibacterial, brain exposure, linezolid, oxazolidinone, sila analogue},
	issn = {1948-5875},
	doi = {10.1021/acsmedchemlett.5b00213},
	author = {Seetharamsingh, B. and Ramesh, Remya and Dange, Santoshkumar S. and Khairnar, Pankaj V. and Singhal, Smita and Upadhyay, Dilip and Veeraraghavan, Sridhar and Viswanadha, Srikant and Vakkalanka, Swaroop and Reddy, D. Srinivasa}
}
@article {42900,
	title = {Repurposing of a drug scaffold: identification of novel sila analogues of rimonabant as potent antitubercular agents},
	journal = {European Journal of Medicinal Chemistry},
	volume = {122},
	year = {2016},
	month = {OCT},
	pages = {723-730},
	abstract = {<p>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.</p>},
	doi = {10.1016/j.ejmech.2016.07.009},
	author = {Ramesh, Remya and Shingare, Rahul D. and Kumar, Vinod and Anand, Amitesh and Swetha, B. and Veeraraghavan, Sridhar and Viswanadha, Srikant and Ummanni, Ramesh and Gokhale, Rajesh S. and Reddy, D. Srinivasa}
}
