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Synthesis and preliminary biological evaluation of a compound library of triazolylcyclitols |
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| Authors: | Gonzalo Carrau Carine C. Drewes Ana Lúcia B. Shimada Ana Bertucci Sandra H.P. Farsky Helio A. Stefani David Gonzalez |
| Affiliation: | 1. Depto. de Química Orgánica, Facultad. de Química, Universidad de la República, UdelaR, Montevideo, Uruguay;2. Departamento de Análises Clínicas e Toxicológicas, Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, São Paulo, SP, Brazil;3. Departamento de Farmácia, Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, São Paulo, SP, Brazil |
| Abstract: | A small library of compounds was prepared by a combination of toluene dioxygenase (TDO)-catalyzed enzymatic dihydroxylation and copper(I)-catalyzed Hüisgen cycloaddition. Some compounds were obtained by coupling an alkyne and a conduritol derivative, while more complex structures were obtained by a double Hüisgen reaction of a dialkyne and two molecules of the cyclitol. The compounds were fully characterized and subjected to preliminary biological screening. |
| Keywords: | Hygromycin Biocatalysis Hüisgen cycloaddition Antifungal Immunosuppressant |
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