e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent

…, SH Choi, JY Park, SH Choi, J Finn, SH Yoon

Index: Im, Weon Bin; Choi, Sun Ho; Park, Ju-Young; Choi, Sung Hak; Finn, John; Yoon, Sung-Hwa European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1027 - 1039

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Citation Number: 62

Abstract

A series of novel substituted pyridyl phenyl oxazolidinone analogues were synthesized and their structure–activity relationship (SAR) was investigated based on in vitro and in vivo antibacterial activities. The minimum inhibitory concentrations (MICs) of the synthesized compounds against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin- resistant enterococci (VRE) ranged from 0.12 to 2.0 μg/mL, and against Haemophilus ...

methyl iodide Structure

5-BROMO-2-(1H-TETRAZOL-5-YL)PYRIDINE Structure

5-BROMO-2-(1H-T...

~0%

5-Bromo-2-(2-methyl-2H-tetrazol-5-yl)-pyridine Structure

5-Bromo-2-(2-me...

5-bromo-2-(1-methyltetrazol-5-yl)pyridine Structure

5-bromo-2-(1-me...

2,5-Dibromopyridine Structure

2,5-Dibromopyridine

~%

5-Bromo-2-(2-methyl-2H-tetrazol-5-yl)-pyridine Structure

5-Bromo-2-(2-me...

5-bromo-2-(1-methyltetrazol-5-yl)pyridine Structure

5-bromo-2-(1-me...

5-Bromo-2-cyanopyridine Structure

5-Bromo-2-cyano...

~%

5-Bromo-2-(2-methyl-2H-tetrazol-5-yl)-pyridine Structure

5-Bromo-2-(2-me...

5-bromo-2-(1-methyltetrazol-5-yl)pyridine Structure

5-bromo-2-(1-me...

Ethanoic anhydride Structure

Ethanoic anhydride

5-BROMO-2-(1H-TETRAZOL-5-YL)PYRIDINE Structure

5-BROMO-2-(1H-T...

~79%

2-(5-bromopyridin-2-yl)-5-methyl-1,3,4-oxadiazole Structure

2-(5-bromopyrid...

2,5-Dibromopyridine Structure

2,5-Dibromopyridine

~%

2-(5-bromopyridin-2-yl)-5-methyl-1,3,4-oxadiazole Structure

2-(5-bromopyrid...

5-Bromo-2-cyanopyridine Structure

5-Bromo-2-cyano...

~%

2-(5-bromopyridin-2-yl)-5-methyl-1,3,4-oxadiazole Structure

2-(5-bromopyrid...

methyl iodide Structure

5-BROMO-2-(1H-TETRAZOL-5-YL)PYRIDINE Structure

5-BROMO-2-(1H-T...

~43%

5-Bromo-2-(2-methyl-2H-tetrazol-5-yl)-pyridine Structure

5-Bromo-2-(2-me...

5-bromo-2-(1-methyltetrazol-5-yl)pyridine Structure

5-bromo-2-(1-me...

2,5-Dibromopyridine Structure

2,5-Dibromopyridine

~%

5-Bromo-2-(2-methyl-2H-tetrazol-5-yl)-pyridine Structure

5-Bromo-2-(2-me...

5-bromo-2-(1-methyltetrazol-5-yl)pyridine Structure

5-bromo-2-(1-me...

5-Bromo-2-cyanopyridine Structure

5-Bromo-2-cyano...

~%

5-Bromo-2-(2-methyl-2H-tetrazol-5-yl)-pyridine Structure

5-Bromo-2-(2-me...

5-bromo-2-(1-methyltetrazol-5-yl)pyridine Structure

5-bromo-2-(1-me...

5-Bromo-2-cyanopyridine Structure

5-Bromo-2-cyano...

~85%

5-BROMO-2-(1H-TETRAZOL-5-YL)PYRIDINE Structure

5-BROMO-2-(1H-T...

2,5-Dibromopyridine Structure

2,5-Dibromopyridine

~%

5-BROMO-2-(1H-TETRAZOL-5-YL)PYRIDINE Structure

5-BROMO-2-(1H-T...

(R)-Glycidyl butyrate Structure

(R)-Glycidyl bu...

4-IODOBENZYLBROMIDE Structure

4-IODOBENZYLBROMIDE

~70%

(|R|)-3-(3-Fluorophenyl)-5-(hydroxymethyl)oxazolidin-2-one Structure

(|R|)-3-(3-Fluo...

3-fluoroaniline Structure

3-fluoroaniline

~%

(5r)-3-(3-fluoro-4-iodophenyl)-5-hydroxymethyloxazolidin-2-one Structure

(5r)-3-(3-fluor...

4-IODOBENZYLBROMIDE Structure

4-IODOBENZYLBROMIDE

~%

(5r)-3-(3-fluoro-4-iodophenyl)-5-hydroxymethyloxazolidin-2-one Structure

(5r)-3-(3-fluor...

Synthesis and antibacterial activity of oxazolidinones conta...

[Jo, Yeong Woo; Im, Weon Bin; Rhee, Jae Keol; Shim, Mi Ja; Kim, Won Bae; Choi, Eung Chil Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 22 p. 5909 - 5915]

Synthesis and antibacterial activity of oxazolidinones conta...

[Jo, Yeong Woo; Im, Weon Bin; Rhee, Jae Keol; Shim, Mi Ja; Kim, Won Bae; Choi, Eung Chil Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 22 p. 5909 - 5915]