کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586935 | 981411 | 2014 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents
ترجمه فارسی عنوان
کشف ترکیبات جدید بیس-اکسازولیدونون به عنوان عوامل بالقوه قوی و انتخابی ضد توتال
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کلمات کلیدی
INHMICMSSAmethicillin-sensitive Staphylococcus aureus - استافیلوکوک اورئوس حساس به متی سیلینMRSA - استافیلوکوک اورئوس مقاوم به متی سیلین یا MRSA methicillin-resistant Staphylococcus aureus - استافیلوکوک اورئوس مقاوم به متیسیلینSelectivity - انتخابیisoniazid - ایزونیازیدTuberculosis - بیماری سلMinimum inhibitory concentration - حداقل غلظت مهاریVero cells - سلول های VeroAntitubercular - ضد تومور
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
A variety of new mono-oxazolidinone molecules by modifying the C-ring of Linezolid, a marketed antibiotic for MRSA, were synthesized and tested for their in vitro antibacterial activities against several Staphylococcus aureus, Mycobacterium smegmatis and two Gram-negative bacteria strains (Escherichia coli and Pseudomonas aeruginosa). Among them, compounds 4-7 displayed moderate antimicrobial activities. After development of a second oxazolidinone ring in the western part of the mono-oxazolidinone compounds 4-7 by a ring closure reaction with N,Nâ²-carbonyldiimidazole (CDI), we found thus obtained bis-oxazolidinone compounds 22-25 possess excellently inhibitory activities against H37Rv but poor or no effects on other test bacteria. Among them, bis-oxazolidinone compound 22 and 24 are the most potent two compounds with a same MIC value of 0.125 μg/mL against H37Rv virulent strain. Compound 22 also exhibited extremely low cytotoxicity on monkey kidney Vero cells with a selective index (IC50/MIC) over 40,000, which suggested bis-oxazolidinone compound 22 is a promising lead compound for subsequent investigation in search of new antitubercular agents.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 6, 15 March 2014, Pages 1496-1501
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 6, 15 March 2014, Pages 1496-1501
نویسندگان
Wei Ang, Weiwei Ye, Zitai Sang, Yuanyuan Liu, Tao Yang, Yong Deng, Youfu Luo, Yuquan Wei,