Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria
A series of novel biaryloxazolidinone derivatives containing amide or acrylamide structure were designed, synthesized and evaluated for their antibacterial activity. [Display omitted] •Biaryloxazolidinone derivatives containing an amide or acrylamide moiety.•Compound 17 exhibited antibacterial activ...
Saved in:
Published in | Bioorganic & medicinal chemistry letters Vol. 29; no. 23; p. 126747 |
---|---|
Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
Published |
OXFORD
Elsevier Ltd
01.12.2019
Elsevier |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | A series of novel biaryloxazolidinone derivatives containing amide or acrylamide structure were designed, synthesized and evaluated for their antibacterial activity.
[Display omitted]
•Biaryloxazolidinone derivatives containing an amide or acrylamide moiety.•Compound 17 exhibited antibacterial activity with MIC values of 0.5 μg/mL against S. aureus, MRSA, MSSA and VRE and 0.25 μg/mL against LREF.•The potency of compound 17 against LREF was 64-fold higher than that of linezolid and 2-fold than that of radezolid.•Compound 17 exhibit higher stability in gastric acid than compound Ⅳ.
A series of novel biaryloxazolidinone derivatives containing amide and acrylamide structure were designed, synthesized and evaluated for their antibacterial activity. Most compounds generally exhibited potent antibacterial activity with MIC values of 1 μg/mL against S. aureus, MRSA, MSSA, LREF and VRE pathogens, using linezolid and radezolid as positive controls. Compound 17 exhibited good antibacterial activity with MIC values of 0.5 μg/mL against S. aureus, MRSA, MSSA and VRE and 0.25 μg/mL against LREF. The results indicated that compound 17 might serve as a potential hit-compound for further investigation. |
---|---|
Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2019.126747 |