کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1365609 981567 2006 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
β-Nitrostyrene derivatives as potential antibacterial agents: A structure–property–activity relationship study
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
β-Nitrostyrene derivatives as potential antibacterial agents: A structure–property–activity relationship study
چکیده انگلیسی

A multidisciplinary project was developed, combining the synthesis of a series of β-nitrostyrene derivatives and the determination of their physicochemical parameters (redox potentials, partition coefficients), to the evaluation of the corresponding antibacterial activity. A complete conformational analysis was also performed, in order to get relevant structural information. Subsequently, a structure–property–activity (SPAR) approach was applied, through linear regression analysis, aiming at obtaining a putative correlation between the physicochemical parameters of the compounds investigated and their antibacterial activity (both against standard strains and clinical isolates). The β-nitrostyrene compounds displayed a lower activity towards all the tested bacteria relative to the β-methyl-β-nitrostyrene analogues. This was observed particularly for the 3-hydroxy-4-methoxy-β-methyl-β-nitrostyrene (IVb) against the Gram-positive bacteria (Staphylococcus aureus, Enterococcus faecalis and Enterococcus faecium). The SPAR results revealed the existence of a clear correlation between the redox potentials and the antibacterial activity of the series of β-nitrostyrene derivatives under study.

An interactive study was developed combining the synthesis of a series of β-nitrostyrene and β-methyl-β-nitrostyrene derivatives and the evaluation of their antibacterial profile, along with the simultaneous determination of some physicochemical parameters, namely their conformational behaviour, redox potential and lipophilicity.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 14, Issue 12, 15 June 2006, Pages 4078–4088
نویسندگان
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