Quinolin-4(1H)-imines are Potent Antiplasmodial Drugs Targeting the Liver Stage of Malaria

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• 作者：Tiago Rodrigues ; Filipa P. da Cruz ; Maria J. Lafuente-Monasterio ; Daniel Gon莽alves ; Ana S. Ressurrei莽茫o ; Ana R. Sitoe ; Maria R. Bronze ; Jiri Gut ; Gisbert Schneider ; Maria M. Mota ; Philip J. Rosenthal ; Miguel Prud锚ncio ; Francisco-Javier Gamo ; Francisca Lopes ; Rui Moreira
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：June 13, 2013
• 年：2013
• 卷：56
• 期：11
• 页码：4811-4815
• 全文大小：241K
• 年卷期：v.56,no.11(June 13, 2013)
• ISSN：1520-4804

文摘

We present a novel series of quinolin-4(1H)-imines as dual-stage antiplasmodials, several-fold more active than primaquine in vitro against Plasmodium berghei liver stage. Among those, compounds 5g and 5k presented low nanomolar IC₅₀ values. The compounds are metabolically stable and modulate several drug targets. These results emphasize the value of quinolin-4(1H)-imines as a new chemotype and their suitable properties for further drug development.