There has been recent interest within this blog in organofluorine moieties in pharmaceuticals. This review discusses the well known aspects of fluorinated drugs, as well as how fluorines can affect protein-ligand binding.
Saturday, September 10, 2011
Fluorine in Pharmaceuticals: Looking Beyond Intuition
There has been recent interest within this blog in organofluorine moieties in pharmaceuticals. This review discusses the well known aspects of fluorinated drugs, as well as how fluorines can affect protein-ligand binding.
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Thanks John, great find! Would you mind summarizing their top 3-5 conclusions in one sentence each? I think that would be great for everyone.
ReplyDeleteAs they mention, it's pretty amazing that 20-30% of all commercial biologically active small molecules are fluorinated, while you don't really find fluorinated compounds in Nature.
So would it be of interest to consider adding fluorination to list of lipinski's rules? Or at least take that into consideration when designing libraries?
ReplyDeleteFragment based libraries could also use some fluorination...???
Adding fluorine into small molecules helps improving the lipophilicity and also helps improving the bioavailability of the small molecules. This is already taken into account in Lipinski's rules: logP < 5. Medicinal chemists often use fluorine functionalities to improve the drug-like properties of lead compounds.
ReplyDeleteSome fragments used in fragment-based libraries already possess fluorine.