کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1357775 981276 2015 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice
ترجمه فارسی عنوان
تحقیق بر روی 4 آمینو 7-کلروکینولین مبتنی بر تیوفن و فوران جدید، ضد مالاریائی را فراهم کرد که موش را درمان می کند
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

We herein report the design and synthesis of a novel series of thiophene- and furan-based aminoquinoline derivatives which were found to be potent antimalarials and inhibitors of β-hematin polymerization. Tested compounds were 3–71 times more potent in vitro than CQ against chloroquine-resistant (CQR) W2 strain with benzonitrile 30 being as active as mefloquine (MFQ), and almost all synthesized aminoquinolines (22/27) were more potent than MFQ against multidrug-resistant (MDR) strain C235. In vivo experiments revealed that compound 28 showed clearance with recrudescence at 40 mg/kg/day, while 5/5 mice survived in Thompson test at 160 mg/kg/day.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 9, 1 May 2015, Pages 2176–2186
نویسندگان
, , , , , , , ,