Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.

Khalaj A; Nakhjiri M; Negahbani AS; Samadizadeh M; Firoozpour L; Rajabalian S; Samadi N; Faramarzi MA; Adibpour N; Shafiee A; Foroumadi A

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Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.

机译：具有强抗革兰氏阳性活性的新型硝基咪唑基-恶唑烷酮杂化物的发现：合成和抗菌评估。

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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.

机译：制备了许多含有硝基芳基-1,3,4-噻二唑部分的利奈唑胺类似物，并将其作为针对一组革兰氏阳性和革兰氏阴性细菌的抗菌剂进行了评估。在合成的化合物中，相对于其他合成的化合物和参考药物利奈唑胺，硝基呋喃类似物1b表现出更强的抑制活性。还使用MTT分析评估了目标化合物对正常小鼠成纤维细胞（NIH / 3T3）细胞的细胞毒活性。结果表明，化合物1c在非细胞毒性浓度下对革兰氏阳性细菌表现出有效的抗菌活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第1期|共6页
作者
Khalaj A; Nakhjiri M; Negahbani AS; Samadizadeh M; Firoozpour L; Rajabalian S; Samadi N; Faramarzi MA; Adibpour N; Shafiee A; Foroumadi A;
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1. Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation. [J] . Khalaj A, Nakhjiri M, Negahbani AS, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第1期

机译：具有强抗革兰氏阳性活性的新型硝基咪唑基-恶唑烷酮杂化物的发现：合成和抗菌评估。
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Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.

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