Selvakumar, N. ; Yadi Reddy, B. ; Sunil Kumar, G. ; Khera, Manoj Kumar ; Srinivas, D. ; Sitaram Kumar, M. ; Das, Jagattaran ; Iqbal, Javed ; Trehan, Sanjay (2006) Synthesis of novel tricyclic oxazolidinones by a tandem SN and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid Bioorganic & Medicinal Chemistry Letters, 16 (16). pp. 4416-4419. 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.2006.05.071
Abstract
A series of conformationally constrained analogues of Linezolid were synthesised by employing a tandem SN2 and SNAr reaction as the key step and tested for antibacterial activity. While the hexahydroazolo-quinoxaline compounds were inactive, the tetrahydroazolo-benzothiazine compounds exhibited interesting antibacterial activity. The introduction of fluorine in the aromatic ring further made the compounds more potent in acetamide compounds resulting in an interesting analogue 32. However, the introduction of fluorine (analogue 34) on the already potent non-fluorine thiocarbamate 21 did not have any influence on the activity.
Item Type: | Article |
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Source: | Copyright of this article belongs to Elsevier Science. |
Keywords: | Oxazolidinones; Antibacterial; Tricyclic; Linezolid |
ID Code: | 17112 |
Deposited On: | 16 Nov 2010 08:28 |
Last Modified: | 17 Feb 2011 04:30 |
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