Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria

  • J Med Chem. 2013 Jun 13;56(11):4811-5. doi: 10.1021/jm400246e.
Tiago Rodrigues  1 ,  Filipa P da Cruz ,  Maria J Lafuente-Monasterio ,  Daniel Gonçalves ,  Ana S Ressurreição ,  Ana R Sitoe ,  Maria R Bronze ,  Jiri Gut ,  Gisbert Schneider ,  Maria M Mota ,  Philip J Rosenthal ,  Miguel Prudêncio ,  Francisco-Javier Gamo ,  Francisca Lopes ,  Rui Moreira
Affiliations
  • 1. Research Institute for Medicines and Pharmaceutical Sciences (iMed.UL), Faculty of Pharmacy, University of Lisbon, Avenida Prof. Gama Pinto, 1649-019 Lisbon, Portugal. [email protected]
PMID: 23701465 DOI: 10.1021/jm400246e
Abstract

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.