Influence of ethylene-Oxy spacer group on the activity of linezolid: Synthesis of potent antibacterials possessing a thiocarbonyl group

…, MS Kumar, S Kandepu, J Das, R Rajagopalan…

Index: Selvakumar; Raheem, Mohammed A.; Khera, Manoj Kumar; Rajale, Trideep V.; Kumar, Magadi Sitaram; Kandepu, Sreenivas; Das, Jagattaran; Rajagopalan; Iqbal, Javed; Trehan, Sanjay Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 23 p. 4169 - 4172

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Citation Number: 13

Abstract

The influence of an ethylene-oxy spacer element between the heterocycle and the aromatic ring in linezolid is reported. The introduction of such spacer group generated compounds with inferior antibacterial activity. However, the conversion of the acetamide group present in the linezolid analogues to either thiocarbamate or thioacetamide functionality restored the activity. The synthesis of linezolid analogues possessing the ethylene-oxy spacer group ...