Modifying Minocycline's Structure to Reduce Risks of Teeth Staining

2009 
Introduced in 1967, minocycline is derived from the tetracycline antibiotics and commonly used to alleviate acne inflammation and to remedy bacterial infections. Antibiotics are generally known to cause side effects, and minocycline is no exception. However, in addition to the allergies, nausea, and headaches, health scientists found the drug to also induce yellow to brown teeth discoloration. Experts attributed this severe side effect to the drug’s inherent chelation with iron cations found in the protein; this strong bind inevitably produces insoluble compounds, which accumulate within the teeth tissues. This study investigated the particular interaction between minocycline and the protein active site, which helped predict more efficacious designs of this drug. Modifications of this molecule were run through Fred receptor, and a pair of fluorine bonds was experimentally proven to be most promising solution to the problem. Modifying Minocycline Structure
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