The presence of fluorine in a pharmaceutical compound can have a profound effect on its bioactivity, stability and lipophilicity, and it is unsurprising that this element is increasingly used in drug design with approximately 25 percent of new commercially available pharmaceuticals containing fluorine atoms. In this paper the application of microorganisms, such as Bacillus, Streptomyces bacteria, and Cunninghamella fungi, in modelling fluorinated drug metabolism in mammals is discussed. The ready scalability of these microbial cultures also provides a platform for the production of drug metabolites for in vitro testing, which is likely to be increasingly important following the US FDA's recent MIST (Metabolites in Safety Testing) guidelines. Furthermore, microorganisms might be employed to identify optimum sites for selective fluorination in iterative drug design.
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