Synthesis and In Vivo Antimalarial Activity of Quinoline/Mercaptopurine Conjugates

Souza, Nicolli Bellotti de; Carvalhaes, Rafael; Carmo, Arturene Maria Lino; Alves, Márcio José Martins; Coimbra, Elaine Soares; Cupolilo, Sônia Maria Neumann; Abramo, Clarice; Silva, Adilson David da

doi:10.2174/157018012799859990

Cited by 7 publications

(2 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Hybrid compounds containing quinolines and anticancer drugs with good antimalarial activity have been reported. De Souza et al prepared quinoline-mercaptopurine hybrid compounds [ 60 ]. The compounds were not cytotoxic at a concentration of 100 μg/mL.…”

Section: Hybrid Compoundsmentioning

confidence: 99%

See 1 more Smart Citation

Quinoline-Based Hybrid Compounds with Antimalarial Activity

2017

View full text Add to dashboard Cite

The application of quinoline-based compounds for the treatment of malaria infections is hampered by drug resistance. Drug resistance has led to the combination of quinolines with other classes of antimalarials resulting in enhanced therapeutic outcomes. However, the combination of antimalarials is limited by drug-drug interactions. In order to overcome the aforementioned factors, several researchers have reported hybrid compounds prepared by reacting quinoline-based compounds with other compounds via selected functionalities. This review will focus on the currently reported quinoline-based hybrid compounds and their preclinical studies.

show abstract

Section: Hybrid Compoundsmentioning

confidence: 99%

“…The compounds were not cytotoxic at a concentration of 100 μg/mL. In vivo evaluation revealed that the compound was effective against P. berghei with over 70% inhibition of parasite multiplication at a dosage of 5 mg/kg/day over a period of 4 days [ 60 ].…”

Section: Hybrid Compoundsmentioning

confidence: 99%

Quinoline-Based Hybrid Compounds with Antimalarial Activity

2017

View full text Add to dashboard Cite

show abstract

Quinoline-based antimalarial hybrid compounds

Vandekerckhove

D’hooghe

2015

Bioorganic & Medicinal Chemistry

192

View full text Add to dashboard Cite

Quinoline-containing compounds, such as quinine and chloroquine, have a long-standing history as potent antimalarial agents. However, the increasing resistance of the Plasmodium parasite against these drugs and the lack of licensed malaria vaccines have forced chemists to develop synthetic strategies toward novel biologically active molecules. A strategy that has attracted considerable attention in current medicinal chemistry is based on the conjugation of two biologically active molecules into one hybrid compound. Since quinolines are considered to be privileged antimalarial building blocks, the synthesis of quinoline-containing antimalarial hybrids has been elaborated extensively in recent years. This review provides a literature overview of antimalarial hybrid molecules containing a quinoline core, covering publications between 2009 and 2014.

show abstract