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South African Journal of Chemistry

On-line version ISSN 1996-840X
Print version ISSN 0379-4350

Abstract

CHIWUNZE, Tirivashe E. et al. Organocatalyzed Mannich Reactions on Minocycline: Towards Novel Tetracycline Antibiotics. S.Afr.j.chem. (Online) [online]. 2016, vol.69, pp.72-78. ISSN 1996-840X.  http://dx.doi.org/10.17159/0379-4350/2016/v69a9.

Herein, we report the development of a mild synthetic route towards novel minocycline derivatives using the proline-catalyzed three-component Mannich reaction. The reaction conditions were optimized and was then screened for its tolerance to the other popular organocatalysts as well as variation of the ketone and aldehyde substrates. The Mannich adducts were evaluated for their in vitro antibacterial efficacies against Gram-negative and Gram-positive bacteria.

Keywords : Minocycline; tetracycline; antibiotics; Mannich reaction; organocatalysis.

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