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

Seetharamsingh, B. ; Ramesh, Remya ; Dange, Santoshkumar S. ; Khairnar, Pankaj V. ; Singhal, Smita ; Upadhyay, Dilip ; Veeraraghavan, Sridhar ; Viswanadha, Srikant ; Vakkalanka, Swaroop ; Reddy, D. Srinivasa (2015) Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure ACS Medicinal Chemistry Letters, 6 (11). pp. 1105-1110. ISSN 1948-5875

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Official URL: http://doi.org/10.1021/acsmedchemlett.5b00213

Related URL: http://dx.doi.org/10.1021/acsmedchemlett.5b00213

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.

Item Type:Article
Source:Copyright of this article belongs to American Chemical Society
ID Code:121945
Deposited On:23 Jul 2021 09:28
Last Modified:23 Jul 2021 09:28

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