Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
A number of linezolid analogues containing a nitroaryl-1,3,4-thiadiazole moiety, were prepared and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Among synthesized compounds, nitrofuran analogue 1b exhibited more potent inhibitory activity, with respect to other synthesized compounds and reference drug linezolid. The target compounds were also assessed for their cytotoxic activity against normal mouse fibroblast (NIH/3T3) cells using MTT assay. The results indicated that compound 1c exhibit potent antibacterial activity against Gram-positive bacteria at non-cytotoxic concentrations.
Department of Medicinal Chemistry, Faculty of Pharmacy & Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Ali
A
Khalaj
Maryam
M
Nakhjiri
Amir Soheil
AS
Negahbani
Marjaneh
M
Samadizadeh
Loghman
L
Firoozpour
Saeed
S
Rajabalian
Nasrin
N
Samadi
Mohammad Ali
MA
Faramarzi
Neda
N
Adibpour
Abbas
A
Shafiee
Alireza
A
Foroumadi
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D055808:Drug Discovery / Q000379:methods*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D051379:Mice; D041681:NIH 3T3 Cells; D009593:Nitroimidazoles / Q000737:chemistry*; D023303:Oxazolidinones / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D009593:Nitroimidazoles; D023303:Oxazolidinones