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Synthesis and properties of macrolones characterized by two ether bonds in the linker.
In this paper synthesis of macrolones 1-18 starting from azithromycin is reported. Two key steps in the construction of the linker between macrolide and quinolone moiety, are formation of centralExpand
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Around the macrolide - Impact of 3D structure of macrocycles on lipophilicity and cellular accumulation.
The aim of this study was to investigate lipophilicity and cellular accumulation of rationally designed azithromycin and clarithromycin derivatives at the molecular level. The effect of substitutionExpand
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Discovery of novel ureas and thioureas of 3-decladinosyl-3-hydroxy 15-membered azalides active against efflux-mediated resistant Streptococcus pneumoniae.
A series of novel ureas and thioureas of 3-decladinosyl-3-hydroxy 15-membered azalides, were discovered, structurally characterized and biologically evaluated. They have shown good antibacterialExpand
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Crystal structures of three substituted pentacyclo[,6.03,10.05,9]undecanes
The crystal structures of three compounds formed via ultimate nucleophilic attack of unsaturated hydrocarbon fragments are reported. Geometries of the bis(vinyl)-, mono(vinyl), andExpand
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Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents.
Malaria remains the most prevalent tropical disease, and due to the spread of resistant parasites novel therapeutics are urgently needed. Azithromycin has shown potential in malaria treatment so weExpand
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Novel 8a-aza-8a-homoerythromycin--4''-(3-substituted-amino)propionates with broad spectrum antibacterial activity.
Fifteen-membered 8a-aza-8a-homoerythromycins derived from either erythromycin or clarithromycin have been acylated to form 4''-O-propenoyl derivative. These functionalized analogues underwent MichaelExpand
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Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides.
Malaria remains one of the most widespread human infectious diseases, and its eradication will largely depend on antimalarial drug discovery. Here, we present a novel approach to the development ofExpand
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Synthesis of macrolones with central piperazine ring in the linker and its influence on antibacterial activity.
Three macrolides, clarithromycin, azithromycin and 11-O-Me-azithromycin have been selected for the construction of a series of new macrolone derivatives. Quinolone-linker intermediates are preparedExpand
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Synthesis and biological activity of 4''-O-acyl derivatives of 14- and 15-membered macrolides linked to omega-quinolone-carboxylic unit.
The synthesis and antimicrobial activity of a new class of macrolide antibiotics which consist of a macrolide scaffold and a quinolone unit covalently connected by an appropriate linker areExpand
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