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A series of 5-substituted oxazolidinones with varying substitution at the 5-position of the oxazolidinone ring were synthesized and their in vitro antibacterial activity was evaluated. The compounds demonstrated potent to weak antibacterial activity. A novel compound (PH-027) demonstrated potent antibacterial activity, which is comparable to or better than those of linezolid and vancomycin against antibiotic-susceptible standard and clinically isolated resistant strains of gram-positive bacteria. Although the presence of the C-5-acetamidomethyl functionality at the C-5 position of the oxazolidinones has been widely claimed and reported as a structural requirement for optimal antimicrobial activity in the oxazolidinone class of compounds, our results from this work identified the C-5 triazole substitution as a new structural alternative for potent antibacterial activity in the oxazolidinone class.
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
December 2003,
Bioorganic & medicinal chemistry letters,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
July 2007,
Chemical biology & drug design,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
September 2009,
Chemical biology & drug design,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
November 2004,
Bioorganic & medicinal chemistry,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
September 2006,
Bioorganic & medicinal chemistry letters,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
August 2007,
European journal of medicinal chemistry,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
October 1973,
Journal of medicinal chemistry,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
July 1987,
Yao xue xue bao = Acta pharmaceutica Sinica,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
May 1998,
Bioorganic & medicinal chemistry letters,
O A Phillips, and
E E Udo, and
A A M Ali, and
N Al-Hassawi
June 1973,
Journal of pharmaceutical sciences,
