Synthesis and biological evaluation of substituted quinolines: potential treatment of protozoal and retroviral co-infections

Fakhfakh, M.; Fournet, Alain; Prina, Éric; Mouscadet, Jean‐François; Franck, Xavier; Hocquemiller, Reynald; Figadère, Bruno

doi:10.1016/j.bmc.2003.09.007

Cited by 181 publications

(100 citation statements)

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“…The 2-substituted quinolines were synthesized in the Laboratory of Pharmacognosy, Faculty of Pharmacy, Chātenay-Malabry, France, by procedures described elsewhere (9). Each compound was shown to have in vitro antileishmanial activity against amastigote forms of L. amazonensis and L. donovani.…”

Section: Methodsmentioning

confidence: 99%

“…In a recent study, Fakhfakh et al (9) described the efficacy of 2-substituted quinolines against both HIV and Leishmania, suggesting that oral therapy with these compounds could treat Leishmania-HIV coinfection.…”

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confidence: 99%

“…From structure-activity relationships, especially those based on the nature of the alkyl chain branched at the 2-position of quinoline, we have selected the compounds with the best in vitro activity as promising drug candidates (9). Therefore, we are interested in establishing simple low-cost methods to prepare these quinolines and deduce in vivo structure-activity relationships.…”

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confidence: 99%

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Efficacy of Orally Administered 2-Substituted Quinolines in Experimental Murine Cutaneous and Visceral Leishmaniases

Nakayama

Loiseau

Bories

et al. 2005

Antimicrob Agents Chemother

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We report in this study the in vivo efficacy of nine 2-substituted quinolines on the Leishmania amazonensis cutaneous infection murine model and on the Leishmania infantum and Leishmania donovani visceral infection murine models. In the case of the L. amazonensis model, quinolines were administered orally at 25 mg/kg twice daily for 15 days. Quinolines 1, 2, 3, and 7 reduced by 80 to 90% the parasite burdens in the lesion, whereas N-methylglucamine antimoniate (Glucantime), administered by subcutaneous injections at 100 mg [28 mg Sb(V)] per kg of body weight daily, reduced the parasite burdens by 98%. In visceral leishmaniasis due to L. infantum, mice treated orally at 25 mg/kg daily for 10 days with quinolines 1, 4, 5, and 6 showed a significant reduction of parasite burdens in the liver and spleen. These quinolines were significantly more effective than meglumine antimoniate to reduce the parasite burden in both the liver and spleen. Also, the oral in vivo activity of three quinolines (quinolines 4, 5, and 2-n-propylquinoline) were determined against L. donovani (LV 9) at 12.5 and 25 mg/kg for 10 days. Their activity was compared with that of miltefosine at 7.5 mg/kg. Miltefosine, 2-n-propylquinoline, and quinoline 5 at 12.5 mg/kg significantly reduced the parasite burdens in the liver by 72, 66, and 61%, respectively. From the present study, quinoline 5 is the most promising compound against both cutaneous and visceral leishmaniasis. The double antileishmanial and antiviral activities of these compounds suggest that this series could be a potential treatment for coinfection of Leishmania-human immunodeficiency virus.

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Section: Methodsmentioning

confidence: 99%

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confidence: 99%

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confidence: 99%

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Efficacy of Orally Administered 2-Substituted Quinolines in Experimental Murine Cutaneous and Visceral Leishmaniases

Nakayama

Loiseau

Bories

et al. 2005

Antimicrob Agents Chemother

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“…A number of metal chelates, as agent for mediation of strand scission of duplex DNA and as chemotherapeutic agents, have been used as probes of DNA structure in solution (4,5) . In medicine particularly , a new class of drugs have been reported as potent HIV-1 inhibitors (6,7) , protein tyrosine kinase inhibitors (8) , protozoal -retroviral co-infections (9) , anti HIV-1 agent (10) and therapeutic drugs for the inflammatory diseases (11) . Looking to the above important of DNA binding study of ligands and metal complexes (12,13) , the present paper describes mixed ligand synthesis and DNA binding interaction assay of L1 and L2.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization, DNA- Binding Interaction studies and antimicrobial screening mixed-ligand Cu (II) and Mn (II) complexes

Al-Obaidi¹

2012

IOSRJAC

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“…Estas sustancias fueron aisladas por primera vez de la quina, extraída de la corteza del árbol de la cinchona, la cual se emplea desde la antigüedad para combatir la malaria, y se encuentran en una gran variedad de moléculas naturales y sinté-ticas que actúan selectivamente frente a algunos protozoos (11)(12)(13)(14).…”

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Compuestos sintéticos tipo estirilquinolinas con actividades leishmanicida y citotóxica

et al. 2014

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Synthesis and biological evaluation of substituted quinolines: potential treatment of protozoal and retroviral co-infections

Cited by 181 publications

References 20 publications

Efficacy of Orally Administered 2-Substituted Quinolines in Experimental Murine Cutaneous and Visceral Leishmaniases

Efficacy of Orally Administered 2-Substituted Quinolines in Experimental Murine Cutaneous and Visceral Leishmaniases

Synthesis, characterization, DNA- Binding Interaction studies and antimicrobial screening mixed-ligand Cu (II) and Mn (II) complexes

Compuestos sintéticos tipo estirilquinolinas con actividades leishmanicida y citotóxica

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