| Literature DB >> 28800458 |
Yuan-Qiang Hu1, Chuan Gao2, Shu Zhang3, Lei Xu2, Zhi Xu2, Lian-Shun Feng4, Xiang Wu5, Feng Zhao6.
Abstract
Malaria, in particular infection with P. falciparum (the most lethal of the human malaria parasite species, responsible for nearly one million deaths every year), is one of the most devastating and common infectious disease throughout the world. Beginning with quinine, quinoline containing compounds have long been used in clinical treatment of malaria and remained the mainstays of chemotherapy against malaria. The emergence of P. falciparum strains resistant to almost all antimalarials prompted medicinal chemists and biologists to study their effective replacement with an alternative mechanism of action and new molecules. Combination with variety of quinolines and other active moieties may increase the antiplasmodial and antimalarial activities and reduce the side effects. Thus, hybridization is a very attractive strategy to develop novel antimalarials. This review aims to summarize the recent advances towards the discovery of antiplasmodial and antimalarial hybrids including quinoline skeleton to provide an insight for rational designs of more active and less toxic quinoline hybrids antimalarials.Entities:
Keywords: Antimalarials; Antiplasmodials; Hybrids; N-contained heterocycles; Quinoline; Quinolone; Structure-activity relationship
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Year: 2017 PMID: 28800458 DOI: 10.1016/j.ejmech.2017.07.061
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514