کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1368979 981737 2015 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and structure–activity relationships of novel cationic lipids with anti-inflammatory and antimicrobial activities
ترجمه فارسی عنوان
سنتز و ساختار فعالیت های مرتبط با لیپیدهای کاتیونی جدید با فعالیت های ضد التهابی و ضد میکروبی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

Certain membrane-active cationic steroids are known to also possess both anti-inflammatory and antimicrobial properties. This combined functionality is particularly relevant for potential therapies of infections associated with elevated tissue damage, for example, cystic fibrosis airway disease, a condition characterized by chronic bacterial infections and ongoing inflammation. In this study, six novel cationic glucocorticoids were synthesized using beclomethasone, budesonide, and flumethasone. Products were either monosubstituted or disubstituted, containing one or two steroidal groups, respectively. In vitro evaluation of biological activities demonstrated dual anti-inflammatory and antimicrobial properties with limited cytotoxicity for all synthesized compounds. Budesonide-derived compounds showed the highest degree of both glucocorticoid and antimicrobial properties within their respective mono- and disubstituted categories. Structure–activity analyses revealed that activity was generally related to the potency of the parent glucocorticoid. Taken together, these data indicate that these types of dual acting cationic lipids can be synthesized with the appropriate starting steroid to tailor activities as desired.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 14, 15 July 2015, Pages 2837–2843
نویسندگان
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