کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369723 981787 2016 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and antimalarial evaluation of novel thiazole derivatives
ترجمه فارسی عنوان
طراحی، سنتز و ارزشیابی ضد مالاریا از مشتقات تازول جدید
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

As part of our medicinal chemistry program’s ongoing search for compounds with antimalarial activity, we prepared a series of thiazole analogs and conducted a SAR study analyzing their in vitro activities against the chloroquine-sensitive Plasmodium falciparum 3D7 strain. The results indicate that modifications of the N-aryl amide group linked to the thiazole ring are the most significant in terms of in vitro antimalarial activity, leading to compounds with high antimalarial potency and low cytotoxicity in HepG2 cell lines. Furthermore, the observed SAR implies that non-bulky, electron-withdrawing groups are preferred at ortho position on the phenyl ring, whereas small atoms such as H or F are preferred at para position. Finally, replacement of the phenyl ring by a pyridine affords a compound with similar potency, but with potentially better physicochemical properties which could constitute a new line of research for further studies.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 16, 15 August 2016, Pages 3938–3944
نویسندگان
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