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Synthesis And In Vitro Antimicrobial Activities Of Novel 7-Substituted 3-Azabicyclo[3.3.0]Octanylphenyl Oxazolidinone Derivatives
Oxazolidinones are a new class of antibacterial agents used to close the innovation gap in the antibacterial drug development to ovecome growing incidence and prevalence of bacterial resistance to clinically useful antibacterials. Linezolid (Figure 1),[1] marketed under the trade name Zyvox􀀀 in 2000, is the first and only oxazolidinone antibacterials approved for the treatment of Gram-positive bacterial infections in humans. Recently, sutezolid, torezolid, radezolid, and ranbezolid,[2] as shown in Figure 1, are under clinical development for the treatment of tuberculosis and skin infection with serious Gram-positive bacterial infections. As an our contineous work [3,4], novel oxazolidinone derivatives having 7-Substituted 3-Azabicyclo[3.3.0]octanyl moieties at the C-ring of linezolid, and acetamide (a) or 1,2,3-triazole (b) ring as C-5 side chain of oxazolidinone ring were prepared and evaluated in vitro antimicrobial activity against Mycobacterium tuberculosis and a panel of clinically important vancomycin-resistant bacteria. Among them, several analogs in this series exhibited potent in vitro antibacterial activity, and especially endo-alcohol 2a and exo-alcohol 2b demonstrated highly potent inhibitory activity against M. tuberculosis H37Rv superior to linezolid. Selected compounds with high antimicrobial activitiy showed good human microsomal stability, CYP-profile, and low monoamine oxidase inhibition
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