Selvakumar, N. ; Govinda Rajulu, G. ; Chandra Shekar Reddy, K. ; Chandra Chary, B. ; Kalyan Kumar, P. ; Madhavi, T. ; Praveena, K. ; Hari Prasada Reddy, K. ; Takhi, Mohammed ; Mallick, Arundhuti ; Amarnath, P. V. S. ; Kandepu, Sreenivas ; Iqbal, Javed (2008) Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality Bioorganic & Medicinal Chemistry Letters, 18 (2). pp. 856-860. ISSN 0960-894X
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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S09608...
Related URL: http://dx.doi.org/10.1016/j.bmcl.2007.09.024
Abstract
The syntheses of a number of novel oxazolidinone analogues possessing an urea functionality are reported. While the urea derivatives possessing aliphatic and aromatic groups were prepared by the more conventional isocyanate method, the derivatives possessing heterocyclic rings were synthesized by a relatively uncommon but otherwise efficient carbamate chemistry. Though the SAR resulted in novel compounds possessing in vitro activity equivalent to Linezolid, the compounds possess a range of substituents that are amenable for altering physicochemical properties of the resultant drug. The antibacterial activity was found to be not sensitive to the functional groups attached to the urea site regardless of the size and electronic characteristics. Based on in vivo results, one molecule has been identified as a candidate and additional work such as salt selection, scale-up, etc., are currently underway to take the molecule further through development.
Item Type: | Article |
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Source: | Copyright of this article belongs to Elsevier Science. |
Keywords: | Oxazolidinones; Antibacterial; Linezolid; Urea |
ID Code: | 17074 |
Deposited On: | 16 Nov 2010 08:34 |
Last Modified: | 17 Feb 2011 04:27 |
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