Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids

Lombard, Marli C.; N’Da, David D.; Breytenbach, Jaco C.; Smith, Peter J.; Lategan, Carmen

doi:10.1016/j.bmcl.2011.01.103

Cited by 38 publications

(21 citation statements)

References 19 publications

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“…Towards these goals, concept of hybrid molecules have been put forward by Meunier and co-workers (27) in malaria chemotherapy, in which two antimalarial pharmacophore are attached covalently, and it is anticipated that these kinds of molecules may solve the problem of drug resistance. In the past few years, number of 4-aminoquinoline-based hybrid molecules are synthesised in an attempt to solve the problem of drug resistance (27)(28)(29)(30)(31)(32)(33)(34)(35)(36).…”

mentioning

confidence: 99%

4‐Aminoquinoline‐Triazine‐Based Hybrids with Improved In Vitro Antimalarial Activity Against CQ‐Sensitive and CQ‐Resistant Strains of Plasmodium falciparum

2013

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A systematic chemical modification in the triazine moiety covalently attached via suitable linkers to 4-amino-7-chloroquinolines yielded a series of new 7-chloro-4-aminoquinoline-triazine hybrids exhibiting high in vitro activity against W2 (chloroquine-resistant) and D6 (chloroquine-sensitive) strains of Plasmodium falciparum without any toxicity against mammalian cell lines (Vero, LLC-PK11, HepG2). Many of the compounds (6, 8, 10, 11, 13, 14, 16, 27, 29 and 33) showed excellent potency against chloroquine sensitive and resistant strains. In particular, compounds 6, 8, 14, 16 and 29 were found to be significantly more active than chloroquine against the chloroquine-resistant strains (W2 clone) of P. falciparum.

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confidence: 99%

4‐Aminoquinoline‐Triazine‐Based Hybrids with Improved In Vitro Antimalarial Activity Against CQ‐Sensitive and CQ‐Resistant Strains of Plasmodium falciparum

2013

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“…4) were equally or more active against P. falciparum CQ-S and CQ-R strains, respectively. The most active hybrid 9a and its oxalate salt were 9-and 7-fold more active than CQ against CQ-R strains (Lombard et al, 2011). Furthermore, in vivo studies of hybrids 9a-9c revealed that they are potentially effective at doses of 1.1, 1.4 and 0.8 (or less) mg/kg/d when administered intraperitoneally (IP), and 12, 16 and 13 mg/kg/d when administered orally.…”

Section: Learning From the Cq Hybrid Approach For Antimalarial Drug Dmentioning

confidence: 98%

Chloroquine-based hybrid molecules as promising novel chemotherapeutic agents

Srivastava

Lee

2015

European Journal of Pharmacology

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“…[17][18] The most potent hybrids exhibited similar in vivo activities to chloroquine (20 nM) against the CQ-susceptible strain of P. falciparum and were superior against the resistant strain (20 vs 160 nM). 19 Furthermore, it appeared that cyclic linkers should not be included and that the linker chain should be limited to two or three carbon atoms with or without methyl substituent.…”

Section: Hybrids Of Quinoline and Artemisinin (Or Derivatives)mentioning

confidence: 99%

“…19 Furthermore, it appeared that cyclic linkers should not be included and that the linker chain should be limited to two or three carbon atoms with or without methyl substituent. [17][18] …”

Section: Hybrids Of Quinoline and Artemisinin (Or Derivatives)mentioning

confidence: 99%

Quinoline-based antimalarial hybrid compounds

Vandekerckhove

D’hooghe

2015

Bioorganic & Medicinal Chemistry

195

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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.

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Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids

Cited by 38 publications

References 19 publications

4‐Aminoquinoline‐Triazine‐Based Hybrids with Improved In Vitro Antimalarial Activity Against CQ‐Sensitive and CQ‐Resistant Strains of Plasmodium falciparum

4‐Aminoquinoline‐Triazine‐Based Hybrids with Improved In Vitro Antimalarial Activity Against CQ‐Sensitive and CQ‐Resistant Strains of Plasmodium falciparum

Chloroquine-based hybrid molecules as promising novel chemotherapeutic agents

Quinoline-based antimalarial hybrid compounds

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