oa South African Journal of Chemistry - Organocatalyzed Mannich reactions on minocycline : towards novel tetracycline antibiotics : research article
|Article Title||Organocatalyzed Mannich reactions on minocycline : towards novel tetracycline antibiotics : research article|
|© Publisher:||South African Chemical Institute (SACI)|
|Journal||South African Journal of Chemistry|
|Affiliations||1 University of KwaZulu-Natal, 2 University of KwaZulu-Natal, 3 University of KwaZulu-Natal, 4 University of KwaZulu-Natal, 5 University of KwaZulu-Natal, 6 University of KwaZulu-Natal, 7 University of KwaZulu-Natal and 8 Karolinska Institutet, Sweden|
|Publication Date||Jan 2016|
|Pages||72 - 78|
|Keyword(s)||Antibiotics, Mannich reaction, Minocycline, Organocatalysis and Tetracycline|
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.
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