Mannich reaction: an approach for the synthesis of water soluble Mulundocandin (cas 108351-20-8) analogues☆☆☆
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Add time:09/06/2019 Source:sciencedirect.com
Semisynthetic modifications at Hydroxy tyrosine (Htyr) unit of Mulundocandin (cas 108351-20-8) (1) were carried out to improve its aqueous solubility. A single step introduction of substituted aminomethyl groups at the ortho position(s) of phenolic hydroxyl of HTyr unit of mulundocandin has been achieved in 7–85% yield. The in vitro screening of Mannich products against Candida albicans and Aspergillus fumigatus, retained the in vivo activity of parent by oral and intraperitoneal route. Compound 20, showed significant improvement in activity over mulundocandin (1) and activity compares well with that of fluconazole.
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