- Characterization and application of a new diprotected cyclam: A novel two-step synthesis of linked tetraazamacrocycles
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The synthesis and separation of the 1,8-di-(tertbutyloxycarbonyl) cyclam (1,8-diboc cyclam) among other isomers allow the facile obtention of singly or doubly linked, and bridged tetraazamacrocycles within a two-step synthesis in a very convenient way. This strategy can be applied to a large scale preparation of several types of dioxygen carriers or activators.
- Boitrel, Bernard,Andrioletti, Bruno,Lachkar, Mohammed,Guilard, Roger
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- Anti-HIV drug and preparation method therefor
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The invention discloses an anti-HIV drug and a preparation method therefor. According to the anti-HIV drug and the preparation method therefor disclosed by the invention, the anti-HIV drug is a Raltegravir derivative ester, the chemical name of which is as follows: N-(2'-(4'-(4'-fluorobenzyl carbamoyl)-1'-methyl-6'-oxo-1',6'-dihydropyrimidine-2'-yl)-5'-methyl-1',3',4'-oxadiazole-2'-formamide-5'-oxy-{5-[1,4,8,11-teraazamacrocycle myristyl]methyl}phenyl)-1,4,8,11-teraazamacrocycle myristyl}-R-carboxylic ester. Compared to Raltegravir, the anti-HIV drug shows obvious and relatively higher activity (EC50) and selectivity index (SI=EC50/CC50), and solubility of the anti-HIV drug is remarkably improved.
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Paragraph 0021
(2016/10/08)
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- New bicyclam-AZT conjugates: Design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor
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We report the synthesis of mono- and bis-tetraazamacrocycle-AZT conjugates. All new compounds were screened for their ability to inhibit HIV- 1 replication in MT4 cell line and were compared to AZT alone. It appears that N-protected covalent prodrugs are
- Dessolin, Jean,Galea, Pascale,Vlieghe, Patrick,Chermann, Jean-Claude,Kraus, Jean-Louis
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p. 229 - 241
(2007/10/03)
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- Syntheses of new unsymmetrical bispolyazamacrocycles
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We report the synthesis of an original unsymmetrical bismacrocycle bearing a carboxylic side-arm. Two different synthetic pathways were investigated, both involving a Schotten-Baumann like reaction. The first route allowed us to obtain a mixture of compounds whilst the second one was direct and non-ambiguous.
- Dessolin,Quelever,Camplo,Kraus
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p. 853 - 856
(2007/10/03)
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