Organocatalyzed Mannich Reactions on Minocycline: Towards Novel Tetracycline Antibiotics
Autor: | Rafiatu Azumah, Thavendran Govender, Tricia Naicker, Melissa Ramtahal, Hendrik G. Kruger, Per I. Arvidsson, Tirivashe E. Chiwunze, Anou M. Somboro |
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Jazyk: | angličtina |
Rok vydání: | 2016 |
Předmět: |
chemistry.chemical_classification
Reaction conditions Ketone biology 010405 organic chemistry medicine.drug_class Tetracycline antibiotics Minocycline 010402 general chemistry biology.organism_classification 01 natural sciences Aldehyde antibiotics 0104 chemical sciences Adduct chemistry medicine Mannich reaction Organic chemistry organocatalysis Bacteria medicine.drug tetracycline |
Zdroj: | South African Journal of Chemistry, Volume: 69, Pages: 72-78, Published: 2016 |
Popis: | 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. |
Databáze: | OpenAIRE |
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