Antibacterial activity in serum of the 3,5-diamino-piperidine translation inhibitors.
نویسندگان
چکیده
Translation inhibitors of the 3,5-diamino-piperidine series act as aminoglycoside mimetics that inhibit bacterial growth. Here we show antibacterial SAR in the presence and absence of serum with a particular focus toward Pseudomonas aeruginosa.
منابع مشابه
Synthesis and SAR of 3,5-diamino-piperidine derivatives: novel antibacterial translation inhibitors as aminoglycoside mimetics.
Aminoglycoside antibiotics target an internal RNA loop within the bacterial ribosomal decoding site. Here, we describe the synthesis and SAR of novel 3,5-diamino-piperidine derivatives as aminoglycoside mimetics, and show they act as inhibitors of bacterial translation and growth.
متن کاملStructure-activity relationships of novel antibacterial translation inhibitors: 3,5-diamino-piperidinyl triazines.
Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole ...
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Aseries of piperidine derivatives was synthesis by the reaction between substituted benzaldhyde ,pentanone-3,and ammonium acetate by refluxining for 1-2 hr in ethanol and the derivatives refluxed with (4,4'-Diaminodiphenyl sulphone) yielded bispiperidine ,the structures of the synthesized compounds were confirmed by spectroscopy analysis , The reported compounds were screened for their antibact...
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We report the structure-guided discovery, synthesis, and initial characterization of 3,5-diamino-piperidinyl triazines (DAPT), a novel translation inhibitor class that targets bacterial rRNA and exhibits broad-spectrum antibacterial activity. DAPT compounds were designed as structural mimetics of aminoglycoside antibiotics which bind to the bacterial ribosomal decoding site and thereby interfer...
متن کاملSynthesis,Characterization, Biological Evaluation and anti corrosion activity of some new bis-piperidone Derivatives
Aseries of piperidine derivatives was synthesis by the reaction between substituted benzaldhyde ,pentanone-3,and ammonium acetate by refluxining for 1-2 hr in ethanol and the derivatives refluxed with (4,4'-Diaminodiphenyl sulphone) yielded bispiperidine ,the structures of the synthesized compounds were confirmed by spectroscopy analysis , The reported compounds were screened for their antibact...
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عنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 18 11 شماره
صفحات -
تاریخ انتشار 2008