کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
11027090 1666323 2018 17 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and anti-mycobacterial activity evaluation of benzofuran-isatin hybrids
ترجمه فارسی عنوان
طراحی، سنتز و ارزیابی فعالیت ضد میکروب هایکتری در هیبرید بنزوفوران-ایزتین
کلمات کلیدی
هیبرید بنزوفوران-ایزتین، ضد میکروب بی سی، ضد سل، مقاوم در برابر چند دارو، ساختار-فعالیت
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
A series of novel benzofuran-isatin hybrids were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities as well as cytotoxicity. Preliminary results indicated that all hybrids with acceptable cytotoxicity in VERO cells exhibited considerable anti-mycobacterial activities against MTB H37Rv and MDR-TB strains. It is worth noting that hybrid 8f with no cytotoxicity towards VERO cells, was found to be the most active compound against MTB H37Rv and MDR-TB. Comparing to the first-line anti-TB agents (rifampicin and isoniazid), hybrid 8f was more active against MDR-TB. However, both the metabolic stability and in vivo pharmacokinetic profiles of 8f were inferior to inhibitor TAM16. Further modification based on hybrid 8f is needed to improve metabolic stability and pharmacokinetic profiles.204
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 159, 5 November 2018, Pages 277-281
نویسندگان
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