Literature DB >> 21220526

In vitro activities of new 2-substituted quinolines against Leishmania donovani.

Philippe M Loiseau1, Suman Gupta, Aditya Verma, Saumya Srivastava, S K Puri, Faten Sliman, Marie Normand-Bayle, Didier Desmaele.   

Abstract

A series of 9 quinolines and 18 styrylquinolines was evaluated for the drugs' in vitro antileishmanial activities and cytotoxicities. The 7-aroylstyrylquinoline scaffold appeared to be the most promising one, with the most interesting compound, no. 35, exhibiting a 50% inhibitory concentration (IC(50)) of 1.2 μM and a selectivity index value of 121.5. Compound 35 was 10-fold and 8-fold more active than miltefosine and sitamaquine, the reference compounds, with selectivity indexes 607-fold and 60-fold higher, respectively.

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Year:  2011        PMID: 21220526      PMCID: PMC3067194          DOI: 10.1128/AAC.01299-10

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  19 in total

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4.  Leishmanicidal activity of racemic +/- 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3,4-dichlorophenoxy]quinoline.

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5.  Structure-activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture.

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6.  Treatment of visceral leishmaniasis.

Authors:  E M Moore; D N Lockwood
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7.  Use of the Kohonen neural network for rapid screening of ex vivo anti-HIV activity of styrylquinolines.

Authors:  Jaroslaw Polanski; Fatima Zouhiri; Laurence Jeanson; Didier Desmaële; Jean d'Angelo; Jean-François Mouscadet; Rafal Gieleciak; Johann Gasteiger; Marc Le Bret
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8.  Synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles as antileishmanial agents.

Authors:  Kalpana Bhandari; Nagarapu Srinivas; Vijay K Marrapu; Aditya Verma; Saumya Srivastava; Suman Gupta
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Review 10.  Chemistry and structure-activity relationship of the styrylquinoline-type HIV integrase inhibitors.

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7.  Inhibition of in vitro Ebola infection by anti-parasitic quinoline derivatives.

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Review 8.  GDP-Mannose Pyrophosphorylase: A Biologically Validated Target for Drug Development Against Leishmaniasis.

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Review 9.  Recent synthetic efforts in the preparation of 2-(3,4)-alkenyl (aryl) quinoline molecules towards anti-kinetoplastid agents.

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Review 10.  The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates.

Authors:  Philippe M Loiseau; Kaluvu Balaraman; Gillian Barratt; Sébastien Pomel; Rémy Durand; Frédéric Frézard; Bruno Figadère
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  10 in total

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