کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1393999 1501124 2015 18 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Antileishmanial activity of quinazoline derivatives: Synthesis, docking screens, molecular dynamic simulations and electrochemical studies
ترجمه فارسی عنوان
فعالیت ضد انعکاسی از مشتقات کوینازولین: سنتز، صفحه نمایش سوکت، شبیه سازی پویا مولکولی و مطالعات الکتروشیمیایی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی


• A quinazoline derivative (H2) as antileishmanial agent with low cytotoxicity was found.
• H2 is active against promastigote and amastigote form of Leishmania mexicana.
• H2 begins its antiparasitic action in less than 1 h, probably by oxidative mechanism.
• H2 probably has a dual mechanism: oxidative stress inductor and DHFR inhibitors.

A series of quinazoline-2,4,6-triamine were synthesized and evaluated in vitro against Leishmania mexicana. Among them, N6-(ferrocenmethyl)quinazolin-2,4,6-triamine (H2) showed activity on promastigotes and intracellular amastigotes, as well as low cytotoxicity in mammalian cells. Docking and electrochemical studies showed the importance of both the ferrocene and the heterocyclic nucleus to the observed activity. H2 is readily oxidized electrochemically, indicating that the mechanism of action probably involves redox reactions.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 92, 6 March 2015, Pages 314–331
نویسندگان
, , , , , , , , ,