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  • Title: Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
    Author: D'Andrea S, Zheng ZB, Denbleyker K, Fung-Tomc JC, Yang H, Clark J, Taylor D, Bronson J.
    Journal: Bioorg Med Chem Lett; 2005 Jun 02; 15(11):2834-9. PubMed ID: 15911264.
    Abstract:
    The synthesis and antibacterial activity of oxazolidinones containing dihydro-1,2-oxazine and 2-pyrazoline ring systems are described. Linezolid analogs utilizing dihydro-1,2-oxazines as morpholine mimics were prepared utilizing a nitrosoamine/diene 4+2 cycloaddition strategy. Pyrazolidine, hexahydro-pyridazine, and 2-pyrazoline analogs more closely related to eperezolid were also prepared. The most active of these new oxazolidinones were the dihydro-1,2-oxazine 6 and the 2-pyrazoline 20 both of which had potency similar to linezolid against a panel of Gram-positive bacteria.
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